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Isoforms Recommended:	K-Ras

Results for "

K-Ras(G12C)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) Apoptosis (6) Drug Derivative (1) Drug Intermediate (1) ERK (6) Ligands for Target Protein for PROTAC (1) MAPKAPK2 (MK2) (1) MEK (1) Mitochondrial Metabolism (1) mTOR (1) p38 MAPK (4) PERK (1) PI3K (3) PROTACs (2) Ras (42) Reactive Oxygen Species (ROS) (2) Reference Standards (1) SOS1 (2)
By Research Areas:	Cancer (46) Neurological Disease (1)
Click Chemistry:	Alkynes (2)

Inhibitors & Agonists

Recombinant Proteins

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153346

Elironrasib 2 Publications Verification RMC-6291	Ras ERK Apoptosis	Cancer
Elironrasib is an orally active and covalent inhibitor of KRAS ^G12C(ON). Elironrasib forms a tri-complex within tumor cells between KRAS ^G12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS ^G12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS ^G12C mutant cells with a median IC₅₀ of 0.11 nM .

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/KRASG12C/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) .

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 .

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-145926

MRTX0902 2 Publications Verification	SOS1 Ras	Neurological Disease Cancer
MRTX0902 is a potent, selective, brain-penetrant, and orally active SOS1 inhibitor with a K_i of 1.9 nM. MRTX0902 disrupts the SOS1:KRASG12C protein-protein interaction (PPI). MRTX0902 can be used in research on pancreatic ductal adenocarcinoma .

HY-12446

K-Ras(G12C) inhibitor 9	Ras	Cancer
K-Ras (G12C) inhibitor 9 is an allosteric inhibitor of the K-Ras (G12C) .

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-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-107841

K-Ras(G12C) inhibitor 6	Ras	Cancer
K-Ras(G12C) inhibitor 6 is a selective and irreversible *K-Ras ^G12C* inhibitor. K-Ras(G12C) inhibitor 6 can be used for the research of lung cancer .

HY-U00416

ARS-1323	Ras	Cancer
ARS-1323 is a KRAS G12C inhibitor. ARS-1323 specifically binds to the cysteine residue on the mutant K-Ras protein, locks it in the GDP-bound conformation, thereby blocking K-Ras activation and downstream signaling pathways. ARS-1323 can be used to investigate the signal transduction mechanisms and growth characteristics of tumor cells driven by K-Ras G12C .

HY-153262

(7R)-Elisrasib (7R)-D3S-001	Ras	Cancer
KRASG12C IN-2 (compound 17) is an orally active KRAS ^G12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice .

HY-164493

KRASG12C IN-13	Ras	Cancer
KRASG12C IN-13 (LY3499446) is a potent KRAS G12C inhibitor. KRASG12C IN-13 is promising for research of advanced solid tumors including non-small cell lung cancer and colorectal cancer .

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-145928B

Divarasib adipate Maximum Cited Publications 6 Publications Verification GDC-6036 adipate	Ras	Cancer
Divarasib (GDC-6036) adipate is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib adipate covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib adipate induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib adipate can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors .

HY-18604

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

HY-126247B

(R)-BI-2852	Drug Derivative Ras	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.

HY-159591

YK-8S	Ras Akt ERK	Cancer
YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .

HY-128771

K-Ras G12C-IN-4	Ras	Cancer
K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRAS ^G12C .

HY-18606

K-Ras G12C-IN-3	Ras	Cancer
K-Ras G12C-IN-3 (Compound VI-5) is an irreversible small molecule inhibitor of mutant *K-Ras G12C. K-Ras G12C-IN-3* can be used in the research of cancers .

HY-U00417

ARS-1630 1 Publications Verification	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.

HY-12408A

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

HY-146223

AZD4625	Ras p38 MAPK PI3K Apoptosis	Cancer
AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase *KRAS^G12C* inhibitor with an IC₅₀ of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRAS^G12C mutations. AZD4625 can be used for the study of KRAS^G12C mutant non-small cell lung cancer .

HY-179403

KRASG12C IN-17	Ras	Cancer
KRASG12C IN-17 is an orally active covalent KRAS ^G12C inhibitor, showing strong inhibitory activity in KRAS ^G12C-mutant cancer cells (NCI-H23 IC₅₀ = 0.7 nM; NCI-H358 IC₅₀ = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRAS ^G12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer .

HY-18605

K-Ras G12C-IN-2	Ras	Cancer
K-Ras G12C-IN-2 is an irreversible covalent *K-Ras G12C* inhibitor.

HY-173252

KRASG12C ligand-1	Ligands for Target Protein for PROTAC Ras	Cancer
KRASG12C ligand-1 is a PROTAC target protein ligand that can be used to synthesize the PROTAC YN14-H (HY-173250). YN14-H is a PROTAC degrader targeting KRAS ^G12C and has antitumor activity .

HY-12408

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

HY-155356A

YN14 (mixture of diastereomers)	PROTACs	Cancer
YN14 mixture of diastereomers is the diastereomers of YN14 (HY-155356). 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 .

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-146223A

(3R,10R,14aS)-AZD4625	Ras PI3K p38 MAPK Apoptosis	Cancer
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase *KRAS^G12C* inhibitor with an IC₅₀ of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRAS^G12C mutations. AZD4625 can be used for the study of KRAS^G12C mutant non-small cell lung cancer .

HY-163594

KRAS-IN-59	Ras	Cancer
K-Ras-IN-58 is a K-RAS inhibitor and shows inhibitory activity against KRAS^G12D, KRAS^G12C and KRAS WT. K-Ras-IN-58 inhibits proliferation of cancer cells .

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-42936

ARS-1620 intermediate	Drug Intermediate	Others
ARS-1620 intermediate is an intermediate in the synthesis of a K-Ras ^G12C inhibitor ARS1620 (HY-U00418) .

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 .

HY-168919

KRASG12C IN-16	Ras Apoptosis p38 MAPK PI3K mTOR	Cancer
KRASG12C IN-16 (Compound SK-17) is a selective, covalent and an orally active KRAS ^G12C inhibitor. KRASG12C IN-16 induces Apoptosis. KRASG12C IN-16 effectively prevents the activation of MAPK and PI3K/mTOR signaling pathways. KRASG12C IN-16 displays anti-tumor activity against pancreatic cancer .

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 .

HY-173047

KRASG12C IN-15	Ras ERK	Cancer
KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRAS ^G12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC₅₀ of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC₅₀ of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRAS ^G12C mutated MIA PaCa-2 with IC₅₀ of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models .

HY-168716

SOS1-IN-17	SOS1 Ras	Cancer
SOS1-IN-17 (Compound 8d) is an orally active inhibitor for *SOS1-KRASG12C* interaction with an IC₅₀ of 5.1 nM. SOS1-IN-17 inhibits ERK phosphorylation in DLD-1 cell with an IC₅₀ of 18 nM. SOS1-IN-17 exhibits anti-proliferative activity in KRASG12C mutated Mia-Paca-2 cell with an IC₅₀ of 0.11 μM. SOS1-IN-17 exhibits antitumor efficacy against pancreatic cancer in mouse model .

HY-W016889R

CFL-137 (Standard)	Reference Standards Ras	Cancer
CFL-137 is a potent KRasG12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer .

HY-153944

*KRAS G12C* inhibitor 60**	Ras	Cancer
KRAS G12C inhibitor 60 (compound 23) is a *Kras-G12C* inhibitor. KRAS G12C inhibitor 60 can be used for the research of lung cancer, colorectal cancer, pancreatic cancer .

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-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-170550

*KRAS G12C* inhibitor 69**	Ras ERK	Cancer
KRAS G12C inhibitor 69 (Compound K09) is the inhibitor for mutant RAS protein *KRASG12C* with an IC₅₀ of 4.36 nM. KRAS G12C inhibitor 69 inhibits the ERK phosphorylation in NCI-H358 and MIA-PACA-2 with an IC₅₀ of 12 nM and 7 nM. KRAS G12C inhibitor 69 inhibits the proliferation of cancer cell NCI-H358 and MIA-PACA-2 with IC₅₀ of 3.15 nM and 2.33 nM .

HY-182883

KRASG12C IN-20	Ras	Cancer
KRASG12C IN-20 is an orally potent KRAS ^G12C inhibitor with an EC₅₀ of 3.9 nM. KRASG12C IN-20 covalently modifies KRAS ^G12C in its inactive GDP-bound state and locks it to block oncogenic signal transduction. KRASG12C IN-20 exhibits significant activity in lung adenocarcinoma xenograft models. KRASG12C IN-20 can be used for research related to lung adenocarcinoma .

HY-179484

KRASG12C IN-19	Reactive Oxygen Species (ROS) ERK	Cancer
KRASG12C IN-19 is a selective and orally active KRAS ^G12C inhibitor. KRASG12C IN-19 exerts potent antiproliferative activity against the KRAS ^G12C-mutant non small cell lung cancer (NSCLC) cell line H358 with an IC₅₀ of 7.6 nM, and effectively suppresses downstream ERK phosphorylation (IC₅₀ = 24.06 nM). KRASG12C IN 19 has no significant inhibitory activity against KRAS ^G12V and KRAS ^G12D-mutant cancer cells (PANC 1, Panc, AsPC 1, and GP2d cells) with IC₅₀ > 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRAS ^G12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. KRASG12C IN 19 can be employed for research in KRAS ^G12C driven cancers, including non small cell lung cancer, pancreatic cancer, and colorectal cancer .

HY-181965

KRAS G12C-IN-78	Ras ERK p38 MAPK	Cancer
KRAS G12C-IN-78 is a selective SWII-binding *KRASG12C* dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits *ERK1/2* phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .

HY-179702

KD36	Ras PERK Akt Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism	Cancer
KD36 is a selective *KRAS-G12C* inhibitor with an IC₅₀ value of 0.92 μM. KD36 can inhibit the phosphorylation of ERK and AKT, induce the accumulation of reactive oxygen species (ROS), reduce mitochondrial membrane potential, thereby leading to apoptosis of KRAS-G12C mutant cells. KD36 can be used in the research of non-small cell lung cancer (NSCLC) .

HY-179404

KRASG12C IN-18	Ras	Cancer
KRASG12C IN-18 is an orally active covalent KRAS ^G12C inhibitor that achieves complete covalent engagement of KRAS ^G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS ^G12C and resistance-associated variants, including KRAS ^G12C/R68S, with low-nanomolar IC₅₀ values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS ^G12C-driven solid tumor and KRAS ^G12C/R68S xenograft models and can be used for colorectal cancer research .

Cat. No.	Product Name		Classification

HY-179403

KRASG12C IN-17		Alkynes
KRASG12C IN-17 is an orally active covalent KRAS ^G12C inhibitor, showing strong inhibitory activity in KRAS ^G12C-mutant cancer cells (NCI-H23 IC₅₀ = 0.7 nM; NCI-H358 IC₅₀ = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRAS ^G12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer .

HY-179404

KRASG12C IN-18		Alkynes
KRASG12C IN-18 is an orally active covalent KRAS ^G12C inhibitor that achieves complete covalent engagement of KRAS ^G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS ^G12C and resistance-associated variants, including KRAS ^G12C/R68S, with low-nanomolar IC₅₀ values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS ^G12C-driven solid tumor and KRAS ^G12C/R68S xenograft models and can be used for colorectal cancer research .

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