Divarasib, also known as GDC-6036 and RG6330, is an orally bioavailable, highly potent and selective KRAS G12C inhibitor, with a median IC50 in the sub-nanomolar range and greater than 18,000-fold selectivity for G12C versus non-G12C cell lines. GDC-6036 demonstrates greater potency and selectivity compared with other KRAS G12C inhibitors in vitro, and complete tumor growth inhibition in multiple KRAS G12C-positive cell lines and in xenograft mouse models. We will highlight the research program that led to the discovery and optimization of GDC-6036, which is currently in clinical development.
MedKoo Cat#: 207187
Name: Divarasib
CAS#: 2417987-45-0 (active atropisomer)
Chemical Formula: C29H32ClF4N7O2
Exact Mass: 621.2242
Molecular Weight: 622.07
Elemental Analysis: C, 55.99; H, 5.19; Cl, 5.70; F, 12.22; N, 15.76; O, 5.14
The following data is based on the product molecular weight 622.07 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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