R428 (Bemcentinib, BGB324)

Chemical Structure : R428

CAS No.: 1037624-75-1

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货号: PC-20336Not For Human Use, Lab Use Only.

R428 (Bemcentinib, BGB324) is potent, selective and orally bioavailable inhibitor of Axl kinase with IC50 of 14 nM.

规格	价格	库存
5 mg	￥980	In stock
10 mg	￥1480	In stock
25 mg	￥2580	In stock
50 mg	￥4280	In stock
100 mg		Get quote

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生物&药学活性

R428 (Bemcentinib, BGB324) is potent, selective and orally bioavailable inhibitor of Axl kinase with IC50 of 14 nM.
R428 inhibits phosphorylation of Akt (Ser473) and Axl (Tyr821) in cell-based activity assays.
R428 exhibits>100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells.
R428 is >100-fold selective for Axl over insulin receptor,EGFR, HER2, and PDGFRβ and kinases of other subfamilies.
R428 (0-3 uM) dose dependently suppresses invasion of both human MDA-MB-231 and murine 4T1 breast cancer cell lines.
R428 (125 mg/kg, BID) suppresses breast cancer metastasis in MDA-MB-231 xenograft and orthotopic 4T1 models.
R428 suppresses angiogenesis in vivo and modulates expression of surrogate markers in tumor tissue.

物理化学性质&存储条件

分子量	506.66
分子式	C30H34N8
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-((7-pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine

参考文献

1. Holland SJ, et al. Cancer Res. 2010 Feb 15;70(4):1544-54.

2. Hector A, et al. Cancer Biol Ther. 2010 Nov 15;10(10):1009-18.

3. Lijnen HR, et al. J Pharmacol Exp Ther. 2011 May;337(2):457-64.