Brivanib (alaninate)

Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ[1].

Product Specifications

CAS Number

[649735-63-7]

Product Name Alternative

BMS-582664

UNSPSC

12352005

Hazard Statement

H302-H360

Target

Autophagy; VEGFR

Type

Reference compound

Related Pathways

Autophagy; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/brivanib-alaninate.html

Purity

99.45

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(O[C@@H](COC1=CN2C(C(OC3=C(C4=C(NC(C)=C4)C=C3)F)=NC=N2)=C1C)C)[C@@H](N)C

Molecular Formula

C22H24FN5O4

Molecular Weight

441.46

Precautions

P264-P270-P280-P330-P405-P501

References & Citations

[1]Bhide RS, et al. Discovery and preclinical studies of (R) -1- (4- (4-fluoro-2-methyl-1H-indol-5-yloxy) -5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy) propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem, 2006, 49 (7), 2143-2146.|[2]Huynh H, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res, 2008, 14 (19), 6146-6153.|[3]Nakamura I, et al. Correction: Brivanib Attenuates Hepatic Fibrosis In Vivo and Stellate Cell Activation In Vitro by Inhibition of FGF, VEGF and PDGF Signaling. PLoS One. 2015 Nov 3;10 (11) :e0142355.