K-Ras Inhibitor

K-Ras Inhibitors (115):

Cat. No.	Product Name	Effect	Purity

HY-114277

Sotorasib	Inhibitor	99.94%
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 is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.

HY-134813

MRTX1133	Inhibitor	99.42%
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D 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.

HY-130149

Adagrasib	Inhibitor	99.93%
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.

HY-126247

BI-2852	Inhibitor	99.57%
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-125817

BI-3406	Inhibitor	99.95%
BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC₅₀ of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.

HY-156819

RMC-9805	Inhibitor	99.73%
RMC-9805 (KRAS G12D inhibitor 18) is a KRAS G12D inhibitor. RMC-9805 is orally active. RMC-9805 inhibits RAS signaling and induces apoptosis in KRAS G12D mutant cancer cells.

HY-160699

DCC-3116	Inhibitor
DCC-3116 is an orally active ULK1/2 inhibitor. DCC-3116 can promote autophagy in lung cancer cells by inhibiting KRAS^G12C signaling, thereby inhibiting the proliferation of lung cancer cells and exerting anti-cancer effects.

HY-162249

ASP6918	Inhibitor
ASP6918 is a potent and orally active KRAS G12C inhibitor with an IC₅₀ value of 0.028 µM. ASP6918 inhibits cell growth. ASP6918 shows antitumor activity.

HY-145928

Divarasib	Inhibitor	99.46%
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC₅₀ of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

HY-114398

BAY-293	Inhibitor
BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC₅₀ of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.

HY-148439

RMC-6236	Inhibitor	99.88%
RMC-6236 (Compound A122) is a potent RAS(ON)^MULTI inhibitor and can be used for the research of cancer.

HY-145926

MRTX0902	Inhibitor	99.45%
MRTX0902 is an orally active and potent SOS1 inhibitor with an IC₅₀ of 46 nM (WO2021127429A1; Example 12-10).

HY-139612

Opnurasib	Inhibitor	98.94%
Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity.

HY-137516

LC-2	Inhibitor
LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC₅₀s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.

HY-153346

RMC-6291	Inhibitor	99.65%
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-U00418

ARS-1620	Inhibitor	99.62%
ARS-1620 is an atropisomeric selective KRAS^G12C inhibitor with desirable pharmacokinetics.

HY-114436

MRTX-1257	Inhibitor	99.14%
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.

HY-114277A

Sotorasib racemate	Inhibitor	98.99%
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-129523

PROTAC K-Ras Degrader-1	Inhibitor	98.05%
PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades K-Ras based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells.

HY-148098

Pan KRas-IN-1	Inhibitor	98.47%
Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors.

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