Search Result
        
            
            
            
                 
                    | Isoforms Recommended: | B-Raf | 
            
            
         
        
            
                Results for "
bRAF V600E
" in MedChemExpress (MCE) Product Catalog:
            
         
        
        
        
            
            
                
                    
                    
                        
                            | Cat. No. | Product Name | Target | Research Areas | Chemical Structure | 
                    
                    
                        
                            
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                                    - HY-137487
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                                                |  | PROTACs
                                                    
                                                        Raf | Cancer |  
                                                | PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells . (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part. |  
 
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                                    - HY-107415
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                                                |  | Raf | Cancer |  
                                                | PLX7922, a RAF inhibitor, can bind with BRAF V600E. PLX7922 inhibits pERK in BRAF V600E cell lines, and activates pERK in mutant NRAS cell lines . |  
 
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                                    - HY-77113
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                                                |  | Raf | Cancer |  
                                                | B-Raf IN 11 (ZINC72115182) is a selective B-Raf V600E inhibitor (IC50=76 nM), shows selectivity for
 B-Raf V600E over B-Raf WT with selectivity of 3.1-fold. B-Raf IN 11 can be used in colorectal cancer research |  
 
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                                    - HY-153341
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                                                | CFT1946 | PROTACs
                                                    
                                                        Raf | Cancer |  
                                                | Tagarafdeg (CFT1946) is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC) degrader of BRAF V600E with a DC50 of 14 nM in A375 cells. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. Tagarafdeg can be used in tumor research  . |  
 
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                                    - HY-E70649
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                                                |  | Raf | Cancer |  
                                                | BRAF is a member of the Raf kinase family of growth signal transduction protein kinases. BRAF has multiple mutants. BRAF V600E is commonly found in melanoma. BRAF V600E Recombinant Human Active Protein Kinase is a recombinant BRAF V600E protein that can be used to study BRAF V600E-related functions . |  
 
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                                    - HY-146442
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                                                |  | Raf | Cancer |  
                                                | BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF  V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases . |  
 
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                                    - HY-146443
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                                                |  | Raf | Cancer |  
                                                | BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF  V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases . |  
 
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                                    - HY-137488
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                                                |  | PROTACs
                                                    
                                                        Raf | Cancer |  
                                                | PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth . |  
 
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                                    - HY-144271
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                                                |  | Raf | Cancer |  
                                                | RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF wt, and bRAF V600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF V600E mutation, respectively . |  
 
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                                    - HY-108887
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                                                |  | Raf | Cancer |  
                                                | Anticancer agent 124 is an orally active, highly selective and potent pan RAF inhibitor. Anticancer agent 124 inhibits MAPK signalling in BRAF V600E, NRAS and KRAS mutant tumor cells . |  
 
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                                    - HY-18972
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                                                | PLX8394;  FORE8394 | Raf | Cancer |  
                                                | PLX8394 is a potent and selective BRaf inhibitor, with an IC50 of appr 5 nM for BRAF V600E. |  
 
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                                    - HY-15199
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                                                | CEP-32496 hydrochloride;  RXDX-105 hydrochloride | Raf | Cancer |  
                                                | Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM. |  
 
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                                    - HY-147405
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                                                | PF-07284890;  ARRY-461 | Raf
                                                    
                                                        ERK | Cancer |  
                                                | Tinlorafenib (PF-07284890) is the orally active inhibitor for BRAF and CRAF with IC50s of 5.8 nM and 4.1 nM. Tinlorafenib (Compound 10) inhibits V600E mutated BRAF and V600K mutanted BRAF with IC50s of 4.25 nM and 2.7 nM. Tinlorafenib can cross the blood brain barrier. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies  . |  
 
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                                    - HY-117707
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                                                |  | Raf | Cancer |  
                                                | EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers  . |  
 
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                                    - HY-51424
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                                                |  | Raf | Cancer |  
                                                | PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf. |  
 
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                                    - HY-18997
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                                                            PLX7904
                                                            
                                                        
                                                        
                                                            
                                                                
                                                                
                                                                
                                                                    3 Publications Verification PB04 | Raf | Cancer |  
                                                | PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAF V600E in mutant RAS expressing cells. |  
 
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                                    - HY-144269
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                                                |  | Raf | Cancer |  
                                                | SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively . |  
 
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                                    - HY-15200
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                                                | CEP-32496;  RXDX-105 | Raf | Cancer |  
                                                | Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM. |  
 
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                                    - HY-14177A
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                                                |  | Raf | Cancer |  
                                                | B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively. |  
 
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                                    - HY-15605
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                                                | LGX818 | Raf | Cancer |  
                                                | Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM). |  
 
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                                    - HY-15767
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                                                | 
                                                        
                                                            TAK-632
                                                            
                                                        
                                                        
                                                            
                                                                
                                                                
                                                                
                                                                    5 Publications Verification | Raf
                                                    
                                                        Aurora Kinase | Cancer |  
                                                | TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF V600E, BRAF WT, respectively. |  
 
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                                    - HY-150250
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                                                |  | Raf | Cancer |  
                                                | B-Raf IN 13 is a BRAF inhibitor with an IC50 of 3.55 nM in BRAF V600E enzyme assay. B-Raf IN 13 has anticaner effects (WO2020261156A1, Example 74) . |  
 
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                                    - HY-14177
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                                                |  | Raf | Cancer |  
                                                | Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively. |  
 
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                                    - HY-12846
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                                                |  | Raf | Cancer |  
                                                | CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRaf V600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively. |  
 
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                                    - HY-18652
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                                                | Ro 5126766;  CH5126766 | MEK
                                                    
                                                        Raf | Cancer |  
                                                | Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF  (IC50: 8.2, 56, 160 nM, and 190 nM, respectively). |  
 
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                                    - HY-18957
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                                                | BGB-283 | EGFR
                                                    
                                                        Raf | Cancer |  
                                                | Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf V600E and EGFR, respectively. |  
 
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                                    - HY-153603
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                                                |  | Raf | Cancer |  
                                                | B-Raf IN 15 (Compound 7) is a BRAF inhibitor. B-Raf IN 15 inhibits BRAF WT and BRAF V600E with IC50s of 2.0 and 0.8 μM. B-Raf IN 15 can be used for the research of cancer . |  
 
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                                    - HY-14660
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                                                | GSK2118436A;  GSK2118436 | Raf | Cancer |  
                                                | Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively . |  
 
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                                    - HY-18957B
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                                                | BGB-283 maleate | EGFR
                                                    
                                                        Raf | Others
                                                    
                                                        Cancer |  
                                                | Lifirafenib (BGB-283) maleate is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf V600E and EGFR, respectively . |  
 
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                                    - HY-12558
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                                                | DP-4978 | Raf
                                                    
                                                        Autophagy | Cancer |  
                                                | LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAF V600E, BRAF WT and CRAF WT with IC50s of 5.8, 9.1 and 15 nM, respectively. |  
 
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                                    - HY-109080
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                                                | HM95573;  GDC-5573;  RG6185 | Raf | Cancer |  
                                                | Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAF v600E and C-RAF respectively . |  
 
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                                    - HY-155942
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                                                |  | p38 MAPK
                                                    
                                                        Raf | Cancer |  
                                                | B-Raf IN 19 (compound 31) is a BRAF inhibitor that inhibits BRAF(WT) and BRAF(V600E) (IC50: 0.57 μM and 0.28 μM, respectively). B-Raf IN 19 inhibits MAPK signaling in melanoma cells . |  
 
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                                    - HY-136567
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                                                |  | Raf | Cancer |  
                                                | TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay . |  
 
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                                    - HY-168125
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                                                |  | JNK | Cancer |  
                                                | JNK-IN-18 (compund 23b) is a JNK1 inhibitor with IC50 of 2 nM, compared to JNK2 and BRAF(V600E) with IC50 of 125 nM and 98 nM, respectively . |  
 
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                                    - HY-15605R
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                                                | LGX818 (Standard) | Reference Standards
                                                    
                                                        Raf | Cancer |  
                                                | Encorafenib (Standard) is the analytical standard of Encorafenib. This product is intended for research and analytical applications. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM). |  
 
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                                    - HY-149517
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                                                |  | EGFR
                                                    
                                                        Raf
                                                    
                                                        Caspase
                                                    
                                                        Bcl-2 Family
                                                    
                                                        Apoptosis | Inflammation/Immunology
                                                    
                                                        Cancer |  
                                                | EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAF V600E, and EGFR T790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency . |  
 
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                                    - HY-126298
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                                                |  | Raf | Cancer |  
                                                | RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF  340D/Y341D, B-RAF V600E and B-RAF WT, respectively . |  
 
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                                    - HY-14660R
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                                                | GSK2118436A (Standard); GSK2118436 (Standard) | Reference Standards
                                                    
                                                        Raf | Cancer |  
                                                | Dabrafenib (Standard) is the analytical standard of Dabrafenib. This product is intended for research and analytical applications. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively . |  
 
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                                    - HY-12057
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                                                            Vemurafenib
                                                            
                                                        
                                                        
                                                            
                                                                
                                                                    Maximum Cited Publications 95 Publications Verification PLX4032;  RG7204;  RO5185426 | Raf
                                                    
                                                        Autophagy | Cancer |  
                                                | Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively  . Vemurafenib induces cell autophagy . |  
 
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                                    - HY-17598
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                                                |  | Oxidative Phosphorylation
                                                    
                                                        Parasite
                                                    
                                                        p38 MAPK
                                                    
                                                        Raf
                                                    
                                                        Apoptosis | Infection
                                                    
                                                        Cancer |  
                                                | Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research   . |  
 
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                                    - HY-12291
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                                                | HMSL 10017-101-1 | Raf | Cancer |  
                                                | HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells. |  
 
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                                    - HY-12847
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                                                |  | Raf
                                                    
                                                        Src
                                                    
                                                        Apoptosis | Cancer |  
                                                | CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity . |  
 
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                                    - HY-115933
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                                                |  | EGFR
                                                    
                                                        Raf | Cancer |  
                                                | EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC50 of 45 nM for BRAF V600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity . |  
 
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                                    - HY-146492
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                                                |  | VEGFR
                                                    
                                                        Raf
                                                    
                                                        Apoptosis | Cancer |  
                                                | VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase . |  
 
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                                    - HY-117273
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                                                |  | Raf
                                                    
                                                        Autophagy | Cancer |  
                                                | AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity . |  
 
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                                    - HY-146491
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                                                |  | VEGFR
                                                    
                                                        Raf
                                                    
                                                        Apoptosis | Cancer |  
                                                | VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase . |  
 
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                                    - HY-169869
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                                                |  | Raf | Cancer |  
                                                | Pan-Raf/RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC50 values of 3.49 nM (BRaf V600E), 8.86 nM (ARaf), 5.78 nM (BRaf WT), and 1.65 nM (CRaf). Pan-Raf/RTK inhibitor 1 exhibits antiproliferative activities against various cancer cell lines and can be utilized in cancer research . |  
 
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                                    - HY-175435
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                                                |  | PROTACs
                                                    
                                                        Raf | Cancer |  
                                                | CST905 is a potent PROTAC degrader of BRAF-V600E with a DC50 of 18 nM. CST905 is suitable for cancer research. (Structure Note: Pink: target protein ligand (HY-41747); Blue: E3 ligase ligand (HY-125845); Black: linker (HY-78378)) . |  
 
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                                    - HY-12057R
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                                                | PLX4032 (Standard); RG7204 (Standard); RO5185426 (Standard) | Reference Standards
                                                    
                                                        Raf
                                                    
                                                        Autophagy | Cancer |  
                                                | Vemurafenib (Standard) is the analytical standard of Vemurafenib. This product is intended for research and analytical applications. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively  . Vemurafenib induces cell autophagy . |  
 
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                                    - HY-107779
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                                                |  | Raf | Cancer |  
                                                | BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases . |  
 
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                                    - HY-15610
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                                                | RG 7421;  MEK inhibitor 1 | MEK
                                                    
                                                        Apoptosis | Cancer |  
                                                | GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM). |  
 
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                                    - HY-174274
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                                                |  | ERK | Cancer |  
                                                | ERK2-IN-6 (Compound 20) is a highly selective ERK1/2 inhibitor with an IC50 value of 7.9 nM for ERK2. ERK2-IN-6 inhibits the proliferation of BRAF V600E mutant cells (IC50=250 nM in A375 cells). ERK2-IN-6 is promising for research of solid tumors, such as BRAF-mutated melanoma . |  
 
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                                    - HY-149380
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                                                |  | Raf | Cancer |  
                                                | Vem-L-Cy5 (compound 3),modified with the NIR fluorophore cyanine-5 (Cy5),is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAF V600E,and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability,and inhibits cell growth of many types of cancer . |  
 
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                                    - HY-173164
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                                                |  | EGFR
                                                    
                                                        Raf
                                                    
                                                        Apoptosis | Cancer |  
                                                | EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAF V600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity . |  
 
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                                    - HY-164474
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                                                |  | MEK | Cancer |  
                                                | DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy . |  
 
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                                    - HY-17598R
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                                                |  | Oxidative Phosphorylation
                                                    
                                                        Reference Standards
                                                    
                                                        Parasite
                                                    
                                                        p38 MAPK
                                                    
                                                        Raf
                                                    
                                                        Apoptosis | Infection
                                                    
                                                        Cancer |  
                                                | Rafoxanide (Standard) is the analytical standard of Rafoxanide. This product is intended for research and analytical applications. Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research   . |  
 
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                                    - HY-155736
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                                                |  | p38 MAPK
                                                    
                                                        EGFR
                                                    
                                                        Raf
                                                    
                                                        CDK
                                                    
                                                        c-Met/HGFR | Cancer |  
                                                | MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR WT IC50=281 nM, c-MET IC50=205 nM, B-RAF WT IC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR T790M IC50=69 nM and B-RAF V600E IC50=83 nM) . |  
 
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                                    - HY-164529
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                                                |  | Raf
                                                    
                                                        Ras
                                                    
                                                        MEK
                                                    
                                                        ERK
                                                    
                                                        VEGFR
                                                    
                                                        Tie
                                                    
                                                        c-Fms | Cancer |  
                                                | SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer . |  
 
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                                    - HY-132844
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                                                | HL-085 | MEK | Cancer |  
                                                | Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRAS G12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer)  . |  
 
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                                    - HY-147825
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                                                |  | EGFR
                                                    
                                                        Raf
                                                    
                                                        Apoptosis | Cancer |  
                                                | EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively . |  
 
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                                    - HY-148059
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                                                | B-Raf IN 10 | Raf | Cancer |  
                                                | Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC50 between 50 and 100 nM. Uplarafenib shows antitumor activity . |  
 
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                                    - HY-150639
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                                                |  | Raf | Cancer |  
                                                | Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of  V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma . |  
 
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                                    - HY-136420
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                                                |  | PROTACs
                                                    
                                                        Raf
                                                    
                                                        Apoptosis | Cancer |  
                                                | SJF-0628 is a RAF PROTAC degrader. SJF-0628 induces targeted degradation of BRAF in various cancer cell lines (colorectal cancer cell lines (Colo-205, LS-411N, HT-29, RKO) and triple-negative breast cancer cell line DU-4475). SJF-0628 decreases pMEK and pErk levels in DU-4475 cells. SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of colorectal cancer and triple-negative breast cancer. (Pink: RAF ligand (HY-12057), Blue: VHL Ligand ( HY-125845), Black: Linker (HY-B0912)) . |  
 
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