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GDP-bound KRAS G12C

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (3) Caspase (1) Isotope-Labeled Compounds (2) p38 MAPK (1) PI3K (1) Ras (17) Reference Standards (1) TNF Receptor (1)
By Research Areas:	Cancer (18)
Click Chemistry:	Alkynes (2)

Inhibitors & Agonists

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-114277

Sotorasib Maximum Cited Publications 109 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) .

HY-130149

Adagrasib 55+ 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 .

HY-145928

Divarasib 5+ Cited Publications GDC-6036	Ras	Cancer
Divarasib (GDC-6036) is an orally active, selective KRAS ^G12C inhibitor with an IC₅₀ of <0.01 μM. Divarasib covalently binds Cys12 in GDP-bound KRAS ^G12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib induces tumor shrinkage and robust tumor growth inhibition in KRAS ^G12C-positive models and cancer cells. Divarasib can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRAS ^G12C-mutated solid tumors .

HY-159852

BBO-10203	PI3K Ras Akt	Cancer
BBO-10203 is a potent inhibitor of PI3Kα and KRAS ^G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS ^G12C with an IC₅₀ of 0.031 nM and an EC₅₀ of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G₁ arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .

HY-19706

ARS-853 5 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-114277R

Sotorasib (Standard) AMG-510 (Standard)	Ras Reference Standards	Cancer
Sotorasib (Standard) is the analytical standard of Sotorasib. This product is intended for research and analytical applications. 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) .

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) .

HY-176785S

MCB-294	Ras Apoptosis p38 MAPK Caspase TNF Receptor	Cancer
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with K_ds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC₅₀s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and 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-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-145928B

Divarasib adipate 5+ Cited Publications 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-114277S2

Sotorasib-d3 AMG-510-d₃	Isotope-Labeled Compounds Ras	Cancer
Sotorasib-d₃ (AMG-510-d₃) is deuterium labeled Sotorasib. 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) .

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-183645

KRAS G12C-IN-79	Ras	Cancer
KRAS G12C-IN-79 is a KRAS ^G12C inhibitor with an IC₅₀ of 1.9 nM. KRAS G12C-IN-79 functionally inhibits the activity of the GDP-bound form of KRAS ^G12C. KRAS G12C-IN-79 can be used for the research of nonsmall cell lung cancer, colon cancer, pancreatic cancer .

HY-181964

KRAS G12C-IN-77		Cancer
KRAS G12C-IN-77 is an orally active and selective KRAS ^G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS ^G12C (IC₅₀ = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS ^G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS ^G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS ^G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .

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-181889

KRAS G12C-IN-75	Ras	Cancer
KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRAS ^G12C inhibitor with an IC₅₀ of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRAS ^G12C alkylation in KRAS ^G12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer .

HY-181716

KRAS G12C-IN-74	Ras Apoptosis	Cancer
KRAS G12C-IN-74 is an orally active, selective KRAS ^G12C inhibitor with a target IC₅₀ of 43.18 nM. KRAS G12C-IN-74 induces G0/G1 cell cycle arrest and apoptosis in KRAS ^G12C-mutant cancer cells. KRAS G12C-IN-74 is applicable for the research of KRAS ^G12C-mutant pancreatic cancer, colorectal cancer and lung cancer .

Cat. No.	Product Name	Chemical Structure

HY-114277S

Sotorasib-d7
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

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) .

HY-176785S

MCB-294
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with K_ds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC₅₀s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .

MCB-294

MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with K_ds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC₅₀s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .

HY-114277S2

Sotorasib-d3
Sotorasib-d₃ (AMG-510-d₃) is deuterium labeled Sotorasib. 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) .

Cat. No.	Product Name		Classification

HY-176785S

MCB-294		Alkynes
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with K_ds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC₅₀s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .

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 .

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