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Sotorasib

Chemical Structure : Sotorasib

CAS No.: 2252403-56-6

Sotorasib (AMG510, AMG-510)

Catalog No.: PC-73069Not For Human Use, Lab Use Only.

Sotorasib (AMG510) is a potent, selective, covalent KRAS G12C inhibitor with p-ERK IC50 of 68 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Sotorasib (AMG510) is a potent, selective, covalent KRAS G12C inhibitor with p-ERK IC50 of 68 nM.
AMG510 showed great promise in the treatment of KRAS p.G12C-mutant tumors both pre-clinically and clinically.
Treatment with AMG 510 led to the regression of KRASG12C tumours and improved the anti-tumour efficacy of chemotherapy and targeted agents.
In immune-competent mice, treatment with AMG 510 resulted in a pro-inflammatory tumour microenvironment and produced durable cures alone as well as in combination with immune-checkpoint inhibitors.

Physicochemical Properties

M.Wt 560.61
Formula C30H30F2N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((S)-4-acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one

References

1. Lanman BA, et al. J Med Chem. 2020 Jan 9;63(1):52-65.

2. Canon J, et al. Nature. 2019 Nov;575(7781):217-223.

3. Ryan MB, et al. Clin Cancer Res. 2020 Apr 1;26(7):1633-1643.

4. McCormick F. Cancer Cell. 2020 Jan 13;37(1):3-4.

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