Bemcentinib

Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer[1][2].

Product Specifications

CAS Number

[1037624-75-1]

Product Name Alternative

R428; BGB324

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

TAM Receptor

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/R428.html

Purity

99.92

Solubility

DMSO : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

NC1=NC(NC2=CC(CC[C@@H](N3CCCC3)CC4)=C4C=C2)=NN1C(N=N5)=CC6=C5C7=CC=CC=C7CCC6

Molecular Formula

C30H34N8

Molecular Weight

506.64

Precautions

H302, H315, H319, H335

References & Citations

[1]Sensi M, et al. Human cutaneous melanomas lacking MITF and melanocyte differentiation antigens express a functional Axl receptor kinase. J Invest Dermatol. 2011 Dec;131 (12) :2448-57.|[2]Holland SJ, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70 (4) :1544-54.|[3]Lijnen HR, et al. Growth arrest-specific protein 6 receptor antagonism impairs adipocyte differentiation and adipose tissue development in mice. J Pharmacol Exp Ther. 2011 May;337 (2) :457-64.