[CAS NO. 2375482-51-0] BI-2852
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PRODUCTS SPECIFICATIONS [2375482-51-0]
Store
Catalog
SLK-S8959
Brand
Selleck
CAS
2375482-51-0
DESCRIPTION [2375482-51-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 516.59 |
| Molecular Formula | C31H28N6O2 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9358 mL | 9.6789 mL | 19.3577 mL |
| 5 mM | 0.3872 mL | 1.9358 mL | 3.8715 mL |
| 10 mM | 0.1936 mL | 0.9679 mL | 1.9358 mL |
| 50 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL |
Description
BI-2852 is a potent inhibitor of that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.
In vitro
BI-2852 is a 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. In doing so, it blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.
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