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Catalog No. T8684   CAS 2296729-00-3
Synonyms: AMG-510

Sotorasib (AMG-510) is a selective and orally bioavailable KRAS G12C covalent inhibitor.

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Sotorasib Chemical Structure
Sotorasib, CAS 2296729-00-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 128.00
25 mg In stock $ 237.00
50 mg In stock $ 393.00
100 mg In stock $ 483.00
500 mg In stock $ 1,080.00
1 g In stock $ 1,430.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 99.88%
Purity: 99.36%
Purity: 99.25%
Purity: 98.91%
Purity: 98.91%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sotorasib (AMG-510) is a selective and orally bioavailable KRAS G12C covalent inhibitor.
In vitro In cellular assays, AMG 510 covalently modified KRASG12C and inhibited KRASG12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines tested but did not inhibit p-ERK in cell lines with various other KRAS mutations.?AMG 510 also selectively impaired viability of KRAS p.G12C mutant cell lines but did not affect cell lines with other KRAS mutations[1].
In vivo In vivo pharmacodynamic assays demonstrated dose- and time-dependent inhibition of KRASG12Csignaling in human pancreatic and NSCLC tumor xenografts.?Covalent modification of KRASG12C by AMG 510 was measured by mass spectrometry and correlated with p-ERK inhibition in tumors.?AMG 510 significantly inhibited the growth of KRAS p.G12C xenografts and resulted in tumor regression.?Combination treatment of AMG 510 with standard-of-care and targeted agents demonstrated enhanced tumor growth inhibition compared to either single agent.?In a syngeneic model of KRAS p.G12C mutant cancer, AMG 510 treatment significantly inhibited tumor growth and caused regression[1].
Synonyms AMG-510
Molecular Weight 560.59
Formula C30H30F2N6O3
CAS No. 2296729-00-3


Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (89.19 mM), sonification is recommended.

H2O: 33.33 mg/mL (59.46 mM), ultrasonic and adjust pH to 11 with NaOH

TargetMolReferences and Literature

1. Karen Rex, et al. Abstract 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics. 2. Marwan Fakih, et al, Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12Cinhibitor, in advanced solid tumors. Journal of Clinical Oncology.


1. Yang N, Fan Z, Sun S, et al.Discovery of highly potent and selective KRASG12C degraders by VHL-recruiting PROTACs for the treatment of tumors with KRASG12C-Mutation.European Journal of Medicinal Chemistry.2023: 115857. 2. Yun S D, Scott E, Moghadamchargari Z, et al.2′-Deoxy Guanosine Nucleotides Alter the Biochemical Properties of Ras.Biochemistry.2023 3. Wu L L, Jiang W M, Liu Z Y, et al.AMG-510 and cisplatin combination increases antitumor effect in lung adenocarcinoma with mutation of KRAS G12C: a preclinical and translational research.Discover Oncology.2023, 14(1): 91. 4. Guo Y, Tian J, Guo Y, et al.Oncogenic KRAS effector USP13 promotes metastasis in non-small cell lung cancer through deubiquitinating β-catenin.Cell Reports.2023, 42(12).

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Reprogramming Compound Library Anti-Pancreatic Cancer Compound Library FDA-Approved Drug Library Anti-Cancer Metabolism Compound Library Anti-Cancer Compound Library MAPK Inhibitor Library

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Sotorasib 2296729-00-3 GPCR/G Protein MAPK Ras AMG510 KRAS covalent regression mutation Inhibitor G12C anti-tumour AMG-510 inhibit GDP-bound AMG 510 phosphorylation NSCLC inhibitor