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kras g12c inhibitor

" in MedChemExpress (MCE) Product Catalog:

標的別:	Akt (6) AMPK (1) Apoptosis (18) Autophagy (1) Caspase (3) CDK (1) Drug Derivative (1) Drug Intermediate (2) Drug Isomer (3) EGFR (1) ERK (18) Fluorescent Dye (1) Galectin (1) Isotope-Labeled Compounds (3) Ligands for Target Protein for PROTAC (1) MEK (2) Mitochondrial Metabolism (1) mTOR (4) p38 MAPK (6) PARP (2) PERK (10) Phosphatase (1) PI3K (7) Potassium Channel (1) PROTACs (5) Raf (4) Ras (177) Reactive Oxygen Species (ROS) (2) Reference Standards (1) Ribosomal S6 Kinase (RSK) (1) SOS1 (11) Tim3 (1) TNF Receptor (2) ULK (1) YAP (1)
研究分野別:	Cancer (190) Inflammation/Immunology (2)
クリックケミストリー:	Alkynes (9)

192

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製品番号	製品名	Target	研究分野	構造式

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-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-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-143589

Glecirasib JAB-21822; kras g12c inhibitor 36	Ras	Cancer
Glecirasib (Compound 1-2; JAB-21822) is an orally active and potent inhibitor of **KRAS G12C*. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. Glecirasib has the potential for the research of KRAS* G12C-mediated cancer .

HY-158107

BBO-8520 1 Publications Verification	Ras	Cancer
BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS ^G12C with high oral availability. BBO-8520 has the characteristics of KRAS ^G12C (OFF) inhibitor and the function of blocking KRAS ^G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS ^G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS ^G12C to the inactive (OFF) state. BBO-8520 can be used for the research of cancer .

HY-132980

Olomorasib 2 Publications Verification kras g12c inhibitor 19	Ras	Cancer
Olomorasib is a potent inhibitor of **KRAS G12C*. Olomorasib significantly inhibits* tumor growth (extracted from patent WO2021118877A1) .

HY-164315

KRAS G12C inhibitor 67	Ras PERK	Cancer
KRAS G12C inhibitor 67 (Example 35) is an orally active **KRAS G12C** inhibitor. KRAS G12C inhibitor 67 inhibits pERK and active KRas. KRAS G12C inhibitor 67 selectively inhibits the growth of various KRAS G12C mutant tumor cell lines. KRAS G12C inhibitor 67 exhibits anticancer activity against esophageal cancer, bladder cancer, colorectal cancer, lung cancer, and pancreatic cancer .

HY-114277A

Sotorasib racemate 1 Publications Verification 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-148098

Pan KRas-IN-1 1 Publications Verification	Ras	Cancer
Pan KRas-IN-1 is a pan *KRas* inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .

HY-128522

ARS-1323-alkyne	Ras	Cancer
ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .

HY-U00418

ARS-1620 10+ Cited Publications	Ras	Cancer
ARS-1620 is an atropisomeric selective KRAS ^G12C inhibitor with desirable pharmacokinetics.

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-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-148261

KRAS G12C inhibitor 56	Ras	Cancer
KRAS G12C inhibitor 56 (compound IC-6) is a potent SOS1 inhibitor with an IC₅₀ of 1.6 nM. KRAS G12C inhibitor 56 can be used in cancer research .

HY-141477

RM-018	Ras	Cancer
RM-018 is a potent, functionally distinct tricomplex KRAS ^G12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRAS ^G12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRAS ^G12C .

HY-153821

PROTAC KRAS G12C degrader-2	Ras PROTACs	Cancer
PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of *K-Ras* protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .

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-125872

KRAS G12C inhibitor 14	Ras	Cancer
KRas G12C inhibitor 14 (Compound 17) is a potent **KRAS G12C** inhibitor (IC₅₀ = 18 nM).

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-143592

KRAS G12C inhibitor 39	Ras	Cancer
KRAS G12C inhibitor 39 is a potent inhibitor of **KRAS G12C*. KRas* is a highly attractable target of the pharmaceutical industry for cancer research. KRAS G12C inhibitor 39 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2019099524A1, compound 494) .

HY-142460

KRAS G12C inhibitor 28	Ras	Cancer
KRAS G12C inhibitor 28 is a **KRAS G12C** inhibitor with an IC₅₀ of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1) .

HY-12446

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

HY-132966

ASP2453 1 Publications Verification	Ras ERK	Cancer
ASP2453 is a potent, selective and orally active **KRAS G12C** inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC₅₀ value of 40 nM.

HY-147636

KRAS G12C inhibitor 55	Ras	Cancer
KRAS G12C inhibitor 55 (Compound 1) is a **KRAS G12C** inhibitor .

HY-142946

KRAS G12C inhibitor 44	Ras	Cancer
KRAS G12C inhibitor 44 (compound 54) is a potent and orally active **KRAS G12C** inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC₅₀s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo .

HY-112494

KRas G12C inhibitor 4	Ras	Cancer
KRas G12C inhibitor 1 is a compound that inhibits **KRas G12C**, extracted from patent US 20180072723 A1.

HY-125873

KRAS G12C inhibitor 15	Ras	Cancer
KRAS G12C inhibitor 15 is a potent **KRAS G12C** inhibitor extracted from patent WO2019110751A1, compound 22, has an IC₅₀ of 5 nM .

HY-142458

KRAS G12C inhibitor 27	Ras	Cancer
KRAS G12C inhibitor 27 is a **KRAS G12C** inhibitor with antitumor effects (WO2021109737) .

HY-142457

KRAS G12C inhibitor 26	Ras	Cancer
KRAS G12C inhibitor 26 is a **KRAS G12C** inhibitor with antitumor effects (WO2021109737) .

HY-163720

KRAS G12C inhibitor 63	Ras Apoptosis	Cancer
KRAS G12C inhibitor 63 (K45) is a **KRAS G12C** inhibitor. KRAS G12C inhibitor 63 can induce Apoptosis. KRAS G12C inhibitor 63 has antitumor activity .

HY-157067

KRAS G12C inhibitor 62	Ras	Cancer
KRAS G12C inhibitor 62 is a **KRAS G12C** inhibitor. KRAS G12C inhibitor 62 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021121367A1) .

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-159611

KRAS G12C inhibitor 68	Ras	Cancer
KRAS G12C inhibitor 68 (compound I-063) is a **KRAS G12C** inhibitor with an IC₅₀ of 7 nM. KRAS G12C inhibitor 68 has anti-tumor activity .

HY-147633

KRAS G12C inhibitor 52	Ras	Cancer
KRAS G12C inhibitor 52 (Compound 7) is a **KRAS G12C** inhibitor .

HY-147632

KRAS G12C inhibitor 51	Ras	Cancer
KRAS G12C inhibitor 51 (example 1) is a **KRAS G12C** inhibitor .

HY-147635

KRAS G12C inhibitor 54	Ras	Cancer
KRAS G12C inhibitor 54 (Compound 1) is a **KRAS G12C** inhibitor .

HY-147634

KRAS G12C inhibitor 53	Ras	Cancer
KRAS G12C inhibitor 53 (Compound 1) is a **KRAS G12C** inhibitor .

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-153461

KRAS G12C inhibitor 58	Ras	Cancer
KRAS G12C inhibitor 58 is a **KRAS G12C** inhibitor, used in cancer research .

HY-142947

KRAS G12C inhibitor 45	Ras	Cancer
KRAS G12C inhibitor 45 (compound 78) is a potent **KRAS G12C** inhibitor .

HY-142478

KRAS G12C inhibitor 29	Ras	Cancer
KRAS G12C inhibitor 29 is a **KRAS G12C** inhibitor extracted from patent WO2021252339A1, compound 3. KRAS G12C inhibitor 29 can be used for the research of cancer .

HY-142481

KRAS G12C inhibitor 30	Ras	Cancer
KRAS G12C inhibitor 30 is a **KRAS G12C** inhibitor extracted from patent WO2021252339A1, compound 2. KRAS G12C inhibitor 30 can be used for the research of cancer .

HY-142485

KRAS G12C inhibitor 31	Ras	Cancer
KRAS G12C inhibitor 31 is a **KRAS G12C** inhibitor extracted from patent WO2021252339A1, compound 1. KRAS G12C inhibitor 31 can be used for the research of cancer .

HY-142490

KRAS G12C inhibitor 33	Ras	Cancer
KRAS G12C inhibitor 33 is a **KRAS G12C** inhibitor extracted from patent WO2021244603A1, compound 1. KRAS G12C inhibitor 33 can be used for the research of cancer .

HY-151968

KRAS G12C inhibitor 57	Ras	Cancer
KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active **KRAS G12C** inhibitor with an IC₅₀ of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .

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-142511

KRAS G12C inhibitor 34	Ras	Cancer
KRAS G12C inhibitor 34 is a **KRAS G12C** inhibitor extracted from patent WO2021239058A1, compound Z1. KRAS G12C inhibitor 34 can be used for the research of cancer .

HY-142948

KRAS G12C inhibitor 46	Ras	Cancer
KRAS G12C inhibitor 46 (compound WX003) is a potent **KRAS G12C** inhibitor .

製品番号	製品名

HY-L260

KRAS Targeted Compound Library

32 compounds

KRAS (Kirsten Rat Sarcoma Viral Oncogene Homolog) is one of the most important oncogenic driver genes in oncology, with high mutation frequencies in pancreatic cancer, non‑small cell lung cancer, and colorectal cancer. For a long time, KRAS was considered "undruggable" due to the lack of suitable small‑molecule binding pockets on its protein surface. In recent years, with the discovery of the switch‑II pocket and the successful approval of KRAS G12C inhibitors, KRAS‑targeted research has achieved groundbreaking progress, which has also spurred a wave of development targeting non‑G12C mutants such as G12D and G12V, as well as upstream and downstream regulatory factors including SOS1 and SHP2.

MCE KRAS Targeted Compound Library contains 32 small‑molecule compounds targeting the KRAS, serving as high‑quality research tools for mechanistic studies of KRAS‑mutant tumors, combination therapy development, resistance mechanism exploration, and high‑throughput drug screening, thereby providing robust support for KRAS‑targeted drug discovery.

製品番号	製品名	Target	研究分野

HY-P2265A

SAH-SOS1A TFA	SOS1 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 .

HY-P2265

SAH-SOS1A	SOS1 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 .

製品番号	製品名	Target	研究分野	Image

HY-P992366

HFB200901	Galectin Tim3	Cancer
HFB200901 is a galectin LGALS9 inhibitor and immunostimulant that can be used in studies related to pancreatic adenocarcinoma, pancreatic intraepithelial neoplasia, KRAS ^G12C-mutant colon cancer, and prostate cancer. HFB200901 disrupts the LGALS9/TIM-3 axis, while blocking the internalization and vacuolization of recombinant LGALS9. HFB200901 reduces the proportion of regulatory T cells (Treg) and enhances dendritic cell activation, thereby inducing polyfunctional and memory CD8 ⁺ T cell responses. HFB200901 inhibits the progression of pancreatic neoplastic lesions and effectively improves the efficacy of PSMA-based vaccination .

製品番号	製品名	構造式

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 .

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) .

HY-114436S

MRTX-1257-d6
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 .

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) .

製品番号	製品名		Classification

HY-128522

ARS-1323-alkyne		Alkynes
ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .

HY-176786

MCB-36		Alkynes
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities K_d ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS ^G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .

HY-159652

KRAS inhibitor-31 1 Publications Verification		Alkynes
KRAS inhibitor-31 (compound 33) is a *KRAS* inhibitor, with K_D (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRas G12V, respectively .

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-134654

MRTX849 analog 24		Alkynes
MRTX849 analog 24 is an alkyne-containing click probe analogue of KRAS G12C inhibitor MRTX849, which is used to research MRTX849 function .

HY-145962A

MRTX-EX185 formic		Alkynes
MRTX-EX185 formic is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 formic can binds both GDP-loaded and active GNP states of *KRAS* and KRAS (G12D). MRTX-EX185 formic exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, **KRAS (G12C)*, KRAS* (Q61H), KRAS (G13D). MRTX-EX185 formic also binds GDP-loaded HRAS. MRTX-EX185 formic can be used to study various RAS-driven tumors (such as pancreatic 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 .

HY-145962

MRTX-EX185		Alkynes
MRTX-EX185 is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 can binds both GDP-loaded and active GNP states of *KRAS* and KRAS (G12D). MRTX-EX185 exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, **KRAS (G12C)*, KRAS* (Q61H), KRAS (G13D). MRTX-EX185 also binds GDP-loaded HRAS. MRTX-EX185 can be used to study various RAS-driven tumors (such as pancreatic 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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