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KRAS-G12C mutant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AMPK (1) Apoptosis (4) ERK (3) MAPKAPK2 (MK2) (1) mTOR (1) p38 MAPK (1) PARP (1) Phosphatase (1) PI3K (1) PROTACs (1) Raf (1) Ras (22) Ribosomal S6 Kinase (RSK) (1)
By Research Areas:	Cancer (26)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

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 .

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 .

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 .

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 .

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 .

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 .

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 .

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 .

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 .

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 .

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 .

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 .

HY-12408

6H05	Ras	Cancer
6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).

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 .

HY-12408A

6H05 TFA	Ras	Cancer
6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).

HY-155356

YN14	PROTACs Ras	Cancer
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective *KRASG12C* degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.

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 .

HY-145020

KRAS G12C inhibitor 23	Ras	Cancer
KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC₅₀ of 491 nM (WO2021218939A1, compound 1) .

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 (K_D: 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 .

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 .

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) (K_d = 195 nM) and KRAS (G12V) (K_d = 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 .

HY-126247

BI-2852	Ras	Cancer
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

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 .

HY-159190

HRX-0233	MAPKAPK2 (MK2)	Cancer
HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .

HY-126247B

(R)-BI-2852	Others	Cancer
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

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KRAS-G12C mutant

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