Search Result
Results for "
VEGFR-IN-1
" in MedChemExpress (MCE) Product Catalog:
14
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-101219
-
|
|
VEGFR
c-Kit
EGFR
|
Cancer
|
|
VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively [1].
|
-
-
- HY-10799
-
|
|
Complement System
|
Cancer
|
|
EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2 .
|
-
-
- HY-136209
-
|
|
VEGFR
|
Cancer
|
|
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2) .
|
-
-
- HY-10374
-
|
SU5416
|
VEGFR
|
Cancer
|
|
Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC50 of 1.23 μM [1].
|
-
-
- HY-109020
-
|
LHA510
|
VEGFR
|
Others
|
|
Acrizanib (LHA510) is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-VEGFR-2 .
|
-
-
- HY-12297
-
|
SurufatINib; HMPL-012
|
FGFR
VEGFR
|
Cancer
|
|
Sulfatinib (Surufatinib) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.
|
-
-
- HY-10981A
-
|
E7080 mesylate
|
VEGFR
FGFR
PDGFR
RET
c-Kit
|
Cancer
|
|
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-N7177
-
|
|
Drug Metabolite
VEGFR
|
Cancer
|
|
Hydroxytanshinone IIA is a hydroxylated metabolite of Tanshinone IIA. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2 .
|
-
-
- HY-P991430
-
|
TB-403
|
VEGFR
|
Cancer
|
|
RO5323441 (TB-403) is a human IgG1 monoclonal antibody (mAb) targeting PLGF. RO5323441 inhibits the binding of human PlGF-1 or PlGF-2 to VEGFR-1 (IC50 values are 0.1 and 0.2 nM, respectively). RO5323441 blocks PlGF-induced VEGFR-1 phosphorylation in Flt-1-transfected HEK293 cells. RO5323441 has antitumor activity [1].
|
-
-
- HY-P991132
-
|
|
VEGFR
|
Cardiovascular Disease
Cancer
|
|
Efclarofusp alfa is a CHO-expressed humanized antibody consisting of VEGFR-1 and VEGFR-2 regions fused to human IgG1 Fc. Efclarofusp alfa is an angiogenesis inhibitor [1].
|
-
-
- HY-10981
-
Lenvatinib
Maximum Cited Publications
67 Publications Verification
E7080
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
|
Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-10337
-
|
BMS-540215
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β [1].
|
-
-
- HY-18711
-
|
MetatINib free base; c-Met INhibitor 2 free base
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
SCR-1481B1 free base, also known as Metatinib free base, is a small molecule receptor kinase inhibitor that targets both c-MET and vascular endothelial growth factor receptor 2 (VEGFR2) .
|
-
-
- HY-10336
-
|
BMS-582664
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
|
-
-
- HY-161843
-
|
|
Necroptosis
RIP kinase
|
Inflammation/Immunology
|
|
Necroptosis-IN-4, a potent necroptosis inhibitor, is a RIP kinase 1 (RIPK1) inhibitor. Necroptosis-IN-4 has no inhibitory activity against RIPK3 and weak inhibitory activity against VEGFR1/2 and PDGFR-α [1].
|
-
-
- HY-P99830
-
|
KH902
|
VEGFR
|
Cardiovascular Disease
|
|
Conbercept (KH902) is a recombinant fusion protein composed of VEGFR-1 (second domain) and VEGFR-2 (third and fourth domains) regions fused to human IgG1 Fc. Conbercept is a vascular endothelial growth factor (VEGF) inhibitor [1].
|
-
-
- HY-10977
-
|
AV-951; KRN951
|
VEGFR
|
Cancer
|
|
Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy [1].
|
-
-
- HY-16135A
-
|
ESK981 tosylate; BOL 303213X tosylate
|
VEGFR
FGFR
|
Others
Cancer
|
|
CEP-11981 (tosylate) (ESK981 (tosylate), BOL 303213X (tosylate)) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects [1].
|
-
-
- HY-10981S1
-
|
E7080-d5
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
|
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-10977A
-
|
AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate
|
VEGFR
|
Cancer
|
|
Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy [1].
|
-
-
- HY-13308
-
|
BAY 73-4506 hydrochloride
|
VEGFR
Autophagy
PDGFR
Raf
RET
|
Cancer
|
|
Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively [1].
|
-
-
- HY-149512
-
|
|
FGFR
VEGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-1 (compound 2b) is an FGFR1/VEGFR2 inhibitor. FGFR1/VEGFR2-IN-1 can be used for cancer research [1].
|
-
-
- HY-10981S
-
|
E7080-d4
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
|
Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-16135
-
|
ESK981; BOL 303213X
|
VEGFR
FGFR
|
Cancer
|
|
CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects [1].
|
-
-
- HY-133980
-
|
|
Drug Metabolite
|
Cancer
|
|
O-Demethyl Lenvatinib is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-12297R
-
|
SurufatINib (Standard); HMPL-012 (Standard)
|
Reference Standards
FGFR
VEGFR
|
Cancer
|
|
Sulfatinib (Standard) is the analytical standard of Sulfatinib. This product is intended for research and analytical applications. Sulfatinib (Surufatinib) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.
|
-
-
- HY-19624
-
|
ACC-789; ZK202650
|
VEGFR
PDGFR
|
Cancer
|
|
NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
|
-
-
- HY-133980A
-
|
|
Drug Metabolite
|
Cancer
|
|
O-Demethyl Lenvatinib hydrochloride is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET. Lenvatinib shows potent antitumor activities [1] .
|
-
-
- HY-10981R
-
|
E7080 (Standard)
|
Reference Standards
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
|
Lenvatinib (Standard) is the analytical standard of Lenvatinib. This product is intended for research and analytical applications. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-10981AR
-
|
E7080 mesylate (Standard)
|
Reference Standards
VEGFR
FGFR
PDGFR
RET
c-Kit
|
Cancer
|
|
Lenvatinib (mesylate) (Standard) is the analytical standard of Lenvatinib (mesylate). This product is intended for research and analytical applications. Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-I0678
-
|
|
Drug Metabolite
PDGFR
|
Cancer
|
|
Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
|
-
-
- HY-10228
-
|
AMG 706
|
c-Kit
VEGFR
|
Cancer
|
|
Motesanib (AMG 706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
-
- HY-10337R
-
|
BMS-540215 (Standard)
|
Reference Standards
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (Standard) is the analytical standard of Brivanib. This product is intended for research and analytical applications. Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β [1].
|
-
-
- HY-112467
-
|
AV-951 hydrate; KRN951 hydrate
|
VEGFR
|
Cancer
|
|
Tivozanib hydrate (AV-951 hydrate; KRN951 hydrate) is the hydrate form of Tivozanib (HY-10977). Tivozanib hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrate exhibits antitumor efficacy [1].
|
-
-
- HY-10229
-
|
AMG 706 Diphosphate
|
c-Kit
VEGFR
|
Cancer
|
|
Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
-
- HY-B0062
-
|
TKI258 lactate hydrate; CHIR-258 lactate hydrate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
|
-
-
- HY-10207
-
|
CHIR-258 lactate; TKI-258 lactate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
|
-
-
- HY-50904
-
|
BIBF 1120
|
PDGFR
VEGFR
FGFR
|
Cancer
|
|
Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-10977R
-
|
|
VEGFR
|
Cancer
|
|
Tivozanib (Standard) is the analytical standard of Tivozanib. This product is intended for research and analytical applications. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy [1].
|
-
-
- HY-10981S2
-
|
E7080-15N,d4
|
VEGFR
c-Kit
FGFR
RET
PDGFR
Isotope-Labeled Compounds
|
Cancer
|
|
Lenvatinib- 15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-120640
-
|
|
VEGFR
PDGFR
|
Cancer
|
|
BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research [1].
|
-
-
- HY-11106
-
|
BIBF 1120 esylate
|
PDGFR
VEGFR
FGFR
|
Cancer
|
|
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-168597
-
|
|
FGFR
Apoptosis
VEGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-3 (Compound 8m) is a dual inhibitor of FGFR1/VEGFR2. FGFR1/VEGFR2-IN-3 exhibits anti-proliferative and anti-migratory activities against cancer cells, and is capable of inducing cell apoptosis [1].
|
-
-
- HY-10336R
-
|
BMS-582664 (Standard)
|
Reference Standards
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (alaninate) (Standard) is the analytical standard of Brivanib (alaninate). This product is intended for research and analytical applications. Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
|
-
-
- HY-10977AR
-
|
|
VEGFR
|
Cancer
|
|
Tivozanib (hydrochloride hydrate) (Standard) is the analytical standard of Tivozanib (hydrochloride hydrate). This product is intended for research and analytical applications. Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy [1].
|
-
-
- HY-13308R
-
|
|
VEGFR
Autophagy
PDGFR
Raf
RET
|
Cancer
|
|
Regorafenib (Hydrochloride) (Standard) is the analytical standard of Regorafenib (Hydrochloride). This product is intended for research and analytical applications. Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively [1].
|
-
-
- HY-W758126
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
(R)-Brivanib alaninate-d4 is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
|
-
-
- HY-10331
-
Regorafenib
Maximum Cited Publications
67 Publications Verification
BAY 73-4506
|
VEGFR
Autophagy
PDGFR
Raf
RET
c-Kit
FGFR
Tie
|
Cancer
|
|
Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity [1].
|
-
-
- HY-164387
-
|
|
EGFR
PDGFR
VEGFR
|
Cancer
|
|
Sutetinib is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo [1].
|
-
-
- HY-10331B
-
|
BAY 73-4506 mesylate
|
VEGFR
PDGFR
RET
Raf
c-Kit
FGFR
Autophagy
Tie
|
Cancer
|
|
Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity [1].
|
-
- HY-10331A
-
|
BAY 73-4506 monohydrate
|
VEGFR
Autophagy
PDGFR
Raf
RET
FGFR
c-Kit
Tie
|
Cancer
|
|
Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity [1].
|
-
- HY-10977S
-
|
AV-951-d6; KRN951-d6
|
Isotope-Labeled Compounds
VEGFR
|
Cancer
|
|
Tivozanib-d6 (AV-951-d6) is deuterium labeled Tivozanib. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy [1] .
|
-
- HY-10230S
-
|
PKC412-d5; CGP 41251-d5
|
Isotope-Labeled Compounds
PKC
Syk
Akt
PKA
c-Kit
|
Cancer
|
|
Midostaurin-d5 is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM [1].
|
-
- HY-10331S1
-
|
BAY 73-4506-13C,d3
|
VEGFR
Autophagy
PDGFR
Raf
RET
|
Cancer
|
|
Regorafenib- 13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
|
-
- HY-50904S2
-
|
BIBF 1120-d8
|
Isotope-Labeled Compounds
PDGFR
VEGFR
FGFR
|
Cancer
|
|
Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-50904S
-
|
BIBF 1120-d3
|
PDGFR
VEGFR
FGFR
|
Cancer
|
|
Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-164387A
-
|
|
EGFR
VEGFR
PDGFR
|
Cancer
|
|
Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo [1].
|
-
- HY-10229R
-
|
AMG 706 Diphosphate (Standard)
|
Reference Standards
c-Kit
VEGFR
|
Cancer
|
|
Motesanib (Diphosphate) (Standard) is the analytical standard of Motesanib (Diphosphate). This product is intended for research and analytical applications. Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
- HY-10207R
-
|
CHIR-258 lactate (Standard); TKI-258 lactate (Standard)
|
Reference Standards
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib (lactate) (Standard) is the analytical standard of Dovitinib (lactate). This product is intended for research and analytical applications. Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
|
-
- HY-50904R
-
|
BIBF 1120 (Standard)
|
Reference Standards
PDGFR
VEGFR
FGFR
|
Cancer
|
|
Nintedanib (Standard) is the analytical standard of Nintedanib. This product is intended for research and analytical applications. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-50904S1
-
|
BIBF 1120-13C,d3
|
Isotope-Labeled Compounds
PDGFR
VEGFR
FGFR
|
Cancer
|
|
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-I0678S
-
|
|
PDGFR
Drug Metabolite
|
Cancer
|
|
Regorafénib N-oxyde-d3(M2) is the deuterium labeled Regorafénib N-oxyde M2 [1]. Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively .
|
-
- HY-11106R
-
|
BIBF 1120 esylate (Standard)
|
Reference Standards
PDGFR
VEGFR
FGFR
|
Cancer
|
|
Nintedanib esylate (Standard) is the analytical standard of Nintedanib esylate. This product is intended for research and analytical applications. Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-10331R
-
|
BAY 73-4506 (Standard)
|
Reference Standards
VEGFR
Autophagy
PDGFR
Raf
RET
c-Kit
FGFR
Tie
|
Cancer
|
|
Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity [1].
|
-
- HY-50905S
-
|
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
|
Dovitinib-d8 is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively [1] .
|
-
- HY-135366
-
|
|
IKK
|
Inflammation/Immunology
|
|
HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .
|
-
- HY-10331AR
-
|
BAY 73-4506 monohydrate (Standard)
|
Reference Standards
VEGFR
Autophagy
PDGFR
Raf
RET
FGFR
c-Kit
Tie
|
Cancer
|
|
Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity [1].
|
-
- HY-149415
-
|
|
RET
FGFR
VEGFR
c-Kit
c-Met/HGFR
PDGFR
Raf
|
Cancer
|
|
Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively [1].
|
-
- HY-I0678S1
-
|
|
Drug Metabolite
|
Cancer
|
|
Regorafénib N-oxyde (M2)- 13C,d3 is the 13C- and deuterium labeled Regorafénib N-oxyde (M2). Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
|
-
- HY-P990088
-
|
|
VEGFR
PD-1/PD-L1
|
Cardiovascular Disease
|
|
Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) fused via the peptide linker 101GGSGGSGGSGGSGGS 115 to the N-terminus of the heavy chain (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain variant L352>A, L353>A. Sotiburafusp alfa is also an angiogenesis inhibitor [1].
|
-
- HY-10230
-
|
PKC412; CGP 41251
|
PKC
VEGFR
c-Kit
NO Synthase
Apoptosis
|
Cancer
|
|
Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM [1] . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
- HY-168114
-
|
|
FLT3
PDGFR
VEGFR
|
Cancer
|
|
Multi-kinase inhibitor 3 (compound 12) is a potent and orally active multikinase inhibitor with IC50 values of 1.59, 1.23, 1.19, 0.59, 0.22, 1.15 nM for FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, PDGFRβ, respectively. Multi-kinase inhibitor 3 shows antiproliferative activity. Multi-kinase inhibitor 3 shows anticancer activity [1].
|
-
- HY-50905
-
|
CHIR-258; TKI258
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
|
Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity [1] .
|
-
- HY-150026
-
|
|
VEGFR
PDGFR
FGFR
c-Kit
Akt
Src
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity [1].
|
-
- HY-112306
-
|
DCC-2618
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
|
Cancer
|
|
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
|
-
- HY-10230R
-
|
PKC412 (Standard); CGP 41251 (Standard)
|
Reference Standards
PKC
VEGFR
c-Kit
NO Synthase
Apoptosis
|
Cancer
|
|
Midostaurin (Standard) is the analytical standard of Midostaurin. This product is intended for research and analytical applications. Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM [1] . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
- HY-50905R
-
|
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
|
Dovitinib (Standard) is the analytical standard of Dovitinib. This product is intended for research and analytical applications. Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity [1] .
|
-
- HY-W751179
-
|
PKC412-13C6; CGP 41251-13C6
|
Isotope-Labeled Compounds
Apoptosis
VEGFR
PKC
c-Kit
NO Synthase
|
Cancer
|
|
Midostaurin- 13C6 (PKC412- 13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM [1] . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
- HY-112306R
-
|
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
|
Cancer
|
|
Ripretinib (Standard) is the analytical standard of Ripretinib. This product is intended for research and analytical applications. Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
|
-
- HY-117991
-
|
|
VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
|
-
- HY-170846
-
|
|
FGFR
VEGFR
Bcr-Abl
FLT3
Cytochrome P450
|
Inflammation/Immunology
|
|
FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model [1].
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99830
-
|
KH902
|
VEGFR
|
Cardiovascular Disease
|
|
Conbercept (KH902) is a recombinant fusion protein composed of VEGFR-1 (second domain) and VEGFR-2 (third and fourth domains) regions fused to human IgG1 Fc. Conbercept is a vascular endothelial growth factor (VEGF) inhibitor [1].
|
-
- HY-P991430
-
|
TB-403
|
VEGFR
|
Cancer
|
|
RO5323441 (TB-403) is a human IgG1 monoclonal antibody (mAb) targeting PLGF. RO5323441 inhibits the binding of human PlGF-1 or PlGF-2 to VEGFR-1 (IC50 values are 0.1 and 0.2 nM, respectively). RO5323441 blocks PlGF-induced VEGFR-1 phosphorylation in Flt-1-transfected HEK293 cells. RO5323441 has antitumor activity [1].
|
-
- HY-P991132
-
|
|
VEGFR
|
Cardiovascular Disease
Cancer
|
|
Efclarofusp alfa is a CHO-expressed humanized antibody consisting of VEGFR-1 and VEGFR-2 regions fused to human IgG1 Fc. Efclarofusp alfa is an angiogenesis inhibitor [1].
|
-
- HY-P990088
-
|
|
VEGFR
PD-1/PD-L1
|
Cardiovascular Disease
|
|
Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) fused via the peptide linker 101GGSGGSGGSGGSGGS 115 to the N-terminus of the heavy chain (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain variant L352>A, L353>A. Sotiburafusp alfa is also an angiogenesis inhibitor [1].
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10981S
-
|
|
|
Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-10230S
-
|
|
|
Midostaurin-d5 is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM [1].
|
-
-
- HY-50904S2
-
|
|
|
Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-50904S1
-
|
|
|
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-10981S1
-
|
|
|
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-10981S2
-
|
|
|
Lenvatinib- 15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-W758126
-
|
|
|
(R)-Brivanib alaninate-d4 is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
|
-
-
- HY-10977S
-
|
|
|
Tivozanib-d6 (AV-951-d6) is deuterium labeled Tivozanib. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy [1] .
|
-
-
- HY-10331S1
-
|
|
|
Regorafenib- 13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
|
-
-
- HY-50904S
-
|
|
|
Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-I0678S
-
|
|
|
Regorafénib N-oxyde-d3(M2) is the deuterium labeled Regorafénib N-oxyde M2 [1]. Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively .
|
-
-
- HY-50905S
-
|
|
|
Dovitinib-d8 is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively [1] .
|
-
-
- HY-I0678S1
-
|
|
|
Regorafénib N-oxyde (M2)- 13C,d3 is the 13C- and deuterium labeled Regorafénib N-oxyde (M2). Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
|
-
-
- HY-W751179
-
|
|
|
Midostaurin- 13C6 (PKC412- 13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM [1] . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
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