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Sotorasib

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

Storage

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.

TargetMolCitations

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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6H05 KRAS G12D inhibitor 14 ARS-1323-alkyne Kras4B G12D-IN-1 Glecirasib TH-Z835 KRAS G12C inhibitor 58 KRAS G12D modulator-1

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Keywords

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

 

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