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KRAS mutations

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37

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145737A
    PROTAC SOS1 degrader-1 TFA

    		PROTACs Ras Cancer
    PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
    PROTAC SOS1 degrader-1 TFA
  • HY-137497
    KRAS inhibitor-9

    		Ras Apoptosis Cancer
    KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
    KRAS inhibitor-9
  • HY-130149
    Adagrasib
    35+ Cited Publications

    MRTX849

    		 Ras Cancer
    Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
    Adagrasib
  • HY-114491A
    Rineterkib hydrochloride

    		ERK Raf Cancer
    Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
    Rineterkib hydrochloride
  • HY-161236
    KRAS ligand 4

    		Molecular Glues Ras Cancer
    KRAS ligand 4 (compound 2) is a bifunctional molecular glue degrader based on SOS1. KRAS ligand 4 reduces downstream signaling markers pERK and pS6 and displays anti-additional activity in cells with multiple KRAS mutations .
    KRAS ligand 4
  • HY-P3129
    KRAS G13D peptide, 25 mer

    		Ras Inflammation/Immunology Cancer
    KRAS G13D peptide, 25 mer, a KRAS activating oncogene mutation peptide, is an immune potentiator extracted from patent WO2018144775A1. KRAS G13D peptide, 25 mer can be used to prepare KRAS vaccine .
    KRAS G13D peptide, 25 mer
  • HY-145737
    PROTAC SOS1 degrader-1

    		PROTACs Ras Cancer
    PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
    PROTAC SOS1 degrader-1
  • HY-168442
    KRAS inhibitor-40

    		Ras PERK Cancer
    KRAS inhibitor-40 (Compound 41) is a KRAS inhibitor that interferes with the KRAS G12C-BRAF complex. KRAS inhibitor-40 inhibits the ERK phosphorylation of KRAS downstream signaling pathway. KRAS inhibitor-40 can inhibit the proliferation of tumor cells with different KRAS mutation types and has antitumor activity .
    KRAS inhibitor-40
  • HY-162444
    KRAS G12D inhibitor 22

    		Ras Cancer
    KRAS G12D inhibitor 22 (compound 6) is a inhibitor of KRAS mutation. KRAS G12D inhibitor 22 has high activity (IC50＜100 nM), good selectivity and low toxicity.KRAS G12D inhibitor 22 can be used in breast cancer research .
    KRAS G12D inhibitor 22
  • HY-137516A
    LC-2 epimer

    		PROTACs Ras Cancer
    LC-2 epimer is a differential isomer of LC-2. LC-2 is a mutation-selective PROTAC depressant for KRAS and contains a ligand for the von Hippel Lindau E3 ligase linked to the KRAS inhibitor MRTX849 .
    LC-2 epimer
  • HY-114491
    Rineterkib

    		ERK Raf Cancer
    Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
    Rineterkib
  • HY-148260
    KRAS G12D inhibitor 16

    		Ras Cancer
    KRAS G12D inhibitor 16 is a KRAS G12D inhibitor. KRAS G12D inhibitor 16 has inhibitory activity against KRAS G12D and KRAS G12D mutation with IC50 value of 0.7 nM and 0.35 μM, respectively. KRAS G12D inhibitor 16 can be used for the research of many malignant tumor, such as pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), non-small cell lung carcinomas (NSCLC) .
    KRAS G12D inhibitor 16
  • HY-144213
    SOS1-IN-10

    		Ras Cancer
    SOS1-IN-10 is a potent SOS1 inhibitor with an IC50 of 13 nM for KRAS G12C-SOS1 (WO2022017519A1, compound 8) .
    SOS1-IN-10
  • HY-144207
    SOS1-IN-9

    		Ras Cancer
    SOS1-IN-9 is a potent SOS1 inhibitor with an IC50 of 116.5 nM for SOS1-KRAS G12C (WO2022028506A1, compound 302) .
    SOS1-IN-9
  • HY-148273
    Setidegrasib

    KRAS G12D inhibitor 17

    		 PROTACs Ras Cancer
    Setidegrasib (KRAS G12D inhibitor 17, Example 8) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib has antitumor effect. (Blue: E3 ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .
    Setidegrasib
  • HY-153662
    TH-Z816

    		Ras Cancer
    TH-Z816 is a reversible inhibitor againstKRAS(G12D)mutation with an IC50 value of 14 μM, which can be used in cancer research .
    TH-Z816
  • HY-134813
    MRTX1133
    20+ Cited Publications

    		 Ras Cancer
    MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
    MRTX1133
  • HY-16662
    Oncrasin-1

    		Ras Apoptosis Cancer
    Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.
    Oncrasin-1
  • HY-168013
    KRASG12C IN-14

    		Ras Cancer
    KRASG12C IN-14 (compound 15) is an inhibitor targeting the KRAS G12C mutation. KRASG12C IN-14 inhibits CYPA-dependent KRAS-BRAF with an IC50 of 0.002 μM. KRASG12C IN-14 inhibits ERK phosphorylation in NCI-H358 cells with an IC50 of 0.002 μM .
    KRASG12C IN-14
  • HY-161233
    BTX-6654

    		PROTACs ERK Cancer
    BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .
    BTX-6654
  • HY-134813A
    MRTX1133 formic

    		Ras Cancer
    MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
    MRTX1133 formic
  • HY-164492
    LSN3074753

    		Raf Cancer
    LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation .
    LSN3074753
  • HY-148278
    BI-0474

    		Ras Cancer
    BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
    BI-0474
  • HY-168012
    Pan-RAS-IN-6

    		Ras Phosphatase Cancer
    Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
    Pan-RAS-IN-6
  • HY-18652A
    Avutometinib potassium

    Ro 5126766 potassium; CH5126766 potassium

    		 Raf MEK Cancer
    Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC) .
    Avutometinib potassium
  • HY-156671A
    RMC-4998 formic

    		Ras PI3K ERK mTOR Apoptosis Cancer
    RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for tumor research .
    RMC-4998 formic
  • HY-156671
    RMC-4998

    		Ras PI3K ERK mTOR Apoptosis Cancer
    RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research .
    RMC-4998
  • HY-19713
    LJI308
    4 Publications Verification

    		 Ribosomal S6 Kinase (RSK) YB-1 Cancer
    LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation .
    LJI308
  • HY-132844
    Tunlametinib

    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) .
    Tunlametinib
  • HY-114277S
    Sotorasib-d7

    AMG-510-d7

    		 Isotope-Labeled Compounds Ras Cancer
    Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
    Sotorasib-d7
  • HY-114277
    Sotorasib
    Maximum Cited Publications
    72 Publications Verification

    AMG-510

    		 Ras Cancer
    Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
    Sotorasib
  • HY-136726
    CGP-82996

    CINK4

    		 CDK Cancer
    GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer .
    CGP-82996
  • HY-173629
    RMC-5127

    		Ras Apoptosis Cancer
    RMC-5127 is an orally active and brain-penetrant mutant-selective tri-complex RAS G12V inhibitor. RMC-5127 non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding . RMC-5127 inhibits the RAS pathway in KRAS G12V mutant cancer cells, reducing cell proliferation and inducing apoptosis. RMC-5127 is promising for research of cancers with RAS mutations, such as non-small cell lung cancer .
    RMC-5127
  • HY-18707
    K-Ras(G12C) inhibitor 12

    		Ras Apoptosis Cancer
    K-Ras(G12C) inhibitor 12 is an irreversible inhibitor of K-Ras(G12C). K-Ras(G12C) inhibitor 12 can alter the nucleotide-binding preference of K-Ras and block its interaction with effector proteins. K-Ras(G12C) inhibitor 12 can reduce cell viability and induce apoptosis in lung cancer cell lines with G12C mutations. K-Ras(G12C) inhibitor 12 has anti-tumor activity .
    K-Ras(G12C) inhibitor 12
  • HY-148409
    MMRi62

    		Ferroptosis Apoptosis Autophagy MDM-2/p53 Cancer
    MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
    MMRi62
  • HY-147245
    Basroparib

    STP1002

    		 PARP Cancer
    Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors .
    Basroparib
  • HY-16909
    Leptomycin B
    5+ Cited Publications

    CI 940; LMB

    		 CRM1 Fungal Antibiotic Infection Cancer
    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle .
    Leptomycin B

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