Bafetinib

Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity[1][2][3].

Product Specifications

CAS Number

[859212-16-1]

Product Name Alternative

INNO-406; NS-187

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Apoptosis; Bcr-Abl; Src

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Bafetinib.html

Purity

99.18

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C(C(F)(F)F)=C1)CN2C[C@@H](N(C)C)CC2)NC3=CC=C(C)C(NC4=NC=CC(C5=CN=CN=C5)=N4)=C3

Molecular Formula

C30H31F3N8O

Molecular Weight

576.62

Precautions

H315, H319, H320

References & Citations

[1]Chen X, et al. Bafetinib Suppresses the Transcription of PD-L1 Through c-Myc in Lung Cancer. Front Pharmacol. 2022 Jun 2;13:897747.|[2]Grace MS, et al. The tyrosine kinase inhibitor bafetinib inhibits PAR2-induced activation of TRPV4 channels in vitro and pain in vivo. Br J Pharmacol. 2014 Aug;171 (16) :3881-94.|[3]Kuroda J, et al. Apoptosis-based dual molecular targeting by INNO-406, a second-generation Bcr-Abl inhibitor, and ABT-737, an inhibitor of antiapoptotic Bcl-2 proteins, against Bcr-Abl-positive leukemia. Cell Death Differ. 2007 Sep;14 (9) :1667-77.