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Results for "

G12C mutant

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

2

Peptides

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18606
    K-Ras G12C-IN-3

    		Ras Cancer
    K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
    K-Ras G12C-IN-3
  • HY-19706
    ARS-853
    4 Publications Verification

    		 Ras Apoptosis Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .
    ARS-853
  • HY-18604
    K-Ras G12C-IN-1

    		Ras Cancer
    K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
    K-Ras G12C-IN-1
  • HY-153346
    RMC-6291
    1 Publications Verification

    		 Ras ERK Apoptosis Cancer
    RMC-6291 is an orally active and covalent inhibitor of KRAS G12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
    RMC-6291
  • HY-164315
    KRAS G12C inhibitor 67

    		Ras Cancer
    KRAS G12C inhibitor 67 (example 35) is a KRAS G12C inhibitor that selectively inhibits the growth of many KRAS G12C mutant tumor cell lines .
    KRAS G12C inhibitor 67
  • HY-145022
    KRAS G12C inhibitor 25

    		Ras Cancer
    KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC50=0.48 nM). From WO2021216770A1 compound 3 .
    KRAS G12C inhibitor 25
  • HY-151287
    KRAS inhibitor-20

    		Ras Cancer
    KRAS inhibitor-20 is a small molecular inhibitor of KRas G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits KRas G12C with the IC50 value <10 nM .
    KRAS inhibitor-20
  • HY-151999
    KRAS G12C inhibitor 65

    		Ras Cancer
    KRAS G12C inhibitor 65 is a potent and covalent KRAS G12C inhibitor that traps KRAS G12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer .
    KRAS G12C inhibitor 65
  • 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-12408
    6H05

    		Ras Cancer
    6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
    6H05
  • HY-159163
    KRASG12C IN-12

    		Ras Cancer
    KRASG12C IN-12 (compound-1) is a KRAS G12C inhibitor. KRASG12C IN-12 (compound-1) can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant .
    KRASG12C IN-12
  • HY-12408A
    6H05 TFA

    		Ras Cancer
    6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
    6H05 TFA
  • HY-114277A
    Sotorasib racemate

    AMG-510 racemate

    		 Ras p38 MAPK Cancer
    Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research .
    Sotorasib racemate
  • HY-U00416
    ARS-1323

    		Ras Cancer
    ARS-1323, the racemate of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
    ARS-1323
  • HY-154959
    AZD4747

    		Ras Cancer
    AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS G12C inhibitor. AZD4747 has the potential to study cancer .
    AZD4747
  • HY-U00417
    ARS-1630

    		Ras Cancer
    ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
    ARS-1630
  • HY-146223
    AZD4625

    		Ras Cancer
    AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
    AZD4625
  • HY-153724
    BI-2865
    2 Publications Verification

    		 Ras Cancer
    BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM) .
    BI-2865
  • HY-P2265
    SAH-SOS1A

    		Ras Cancer
    SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
    SAH-SOS1A
  • HY-P2265A
    SAH-SOS1A TFA

    		Ras Cancer
    SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
    SAH-SOS1A TFA
  • HY-154313
    Spiclomazine

    Clospirazine

    		 Ras Cancer
    Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .
    Spiclomazine
  • HY-154959A
    (9R,12aR)-AZD4747

    		Others Cancer
    (9R,12aR)-AZD4747 is a diastereomer of AZD4747 (HY-154959). AZD4747 is a selective mutant GTPase KRAS G12C inhibitor with blood-brain barrier permeability. AZD4747 has the potential to study cancer .
    (9R,12aR)-AZD4747
  • HY-156529
    pan-KRAS-IN-2

    		Ras Cancer
    pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively .
    pan-KRAS-IN-2
  • HY-164389
    SML-10-70-1

    		Ras Cancer
    SML-10-70-1 is a ligand for RAS, which covalently modifies the K-Ras G12C mutant protein, and inhibits the phosphorylation of ERK and Akt. SML-10-70-1 inhibits the proliferation of cancer cells H23, H358 and A549 with IC50 of 26.6-47.6 μM .
    SML-10-70-1
  • HY-146223A
    (3R,10R,14aS)-AZD4625

    		Others Cancer
    (3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
    (3R,10R,14aS)-AZD4625
  • HY-153663
    TH-Z827

    		Ras Cancer
    TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM .
    TH-Z827
  • HY-122914
    KRAS inhibitor-3

    		Ras Cancer
    KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
    KRAS inhibitor-3
  • HY-160023
    D3S-001

    		Ras Cancer
    D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. D3S-001 exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
    D3S-001
  • HY-156498
    RMC-7977

    		Ras ERK Raf Ribosomal S6 Kinase (RSK) AMPK Apoptosis PARP Cancer
    RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
    RMC-7977
  • 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-151571
    ZG1077

    		Ras Cancer
    ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC) .
    ZG1077
  • HY-132979
    KRAS G12C inhibitor 18

    		Ras Cancer
    KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities .
    KRAS G12C inhibitor 18
  • HY-114436
    MRTX-1257
    4 Publications Verification

    		 Ras Cancer
    MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
    MRTX-1257
  • HY-114436S
    MRTX-1257-d6

    		Isotope-Labeled Compounds Cancer
    MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
    MRTX-1257-d6
  • HY-130149
    Adagrasib
    Maximum Cited Publications
    30 Publications Verification

    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

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