BI-2852 is a potent KRAS inhibitor that binds with nanomolar affinity to a pocket, thus far perceived to be "undruggable," between switch I and II on RAS. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitors because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
MedKoo Cat#: 207121
Name: BI-2852
CAS#: 2375482-51-0
Chemical Formula: C31H28N6O2
Exact Mass: 516.2274
Molecular Weight: 516.61
Elemental Analysis: C, 72.07; H, 5.46; N, 16.27; O, 6.19
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
DMSO | 77.5 | 150.02 | |
Ethanol | 23.0 | 44.52 |
The following data is based on the product molecular weight 516.61 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 |