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 is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors1,2.
Product Specifications
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.
Purity
≥ 90%
Format
Powder.
Solubility
Soluble in DMSO up to 50 mg/mL. In H20, up to 33.33 mg/mL.
Molecular Formula
C30H30F2N6O3
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, stored under nitrogenIn solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Calculated Molecular Weight
560.59 Da
CAS Number
2296729-00-3
Curated Selection
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