BI-882370

BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases[1].

Product Specifications

CAS Number

[1392429-79-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Raf

Type

Reference compound

Related Pathways

MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bi-882370.html

Concentration

10mM

Purity

99.16

Solubility

DMSO : 17.86 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

CCCS(=O)(NC1=CC=C(F)C(N2C=C(C3=CN=CN=C3)C4=NC(N(C5CCN(CC)CC5)C)=CC=C42)=C1F)=O

Molecular Formula

C28H33F2N7O2S

Molecular Weight

569.67

Precautions

H302, H315, H319

References & Citations

[1]Waizenegger IC, et al. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15 (3) :354-65.