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Background: It is well established that RAS mutations are responsible for more than 30% of human cancers. KRAS(G12C) is the most frequent mutation, found in lung and colon carcinomas. Recent studies uncovered a small molecule called AMG510 (Amgen), or Sotorasib, that inhibits the KRAS(G12C)-mediated signaling pathway by locking the KRAS conformation in the GDP-bound state. Compounds that block the nucleotide exchange (GDP to GTP) reaction in KRAS could lead to the inhibition of tumor cell proliferation in KRAS(G12C)-driven tumors.
CAS Number: 2296729-00-3
Description: 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 is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors1,2.
Format: Powder.
Purity: ≥90%
Storage Stability: -20°C, stored under nitrogenIn solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Target: KRAS G12C
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Fakih, et al., 2019 Journal of Clinical Oncology 37(15): 3003.2. Rex, et al., 2019 Cancer Res. 79(13): 3090.
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