Bemcentinib (R428, BGB324)

Chemical Structure : Bemcentinib

CAS No.: 1037624-75-1

加入收藏

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

Bemcentinib (R428, BGB324) is potent, selective and orally bioavailable inhibitor of Axl kinase with IC50 of 14 nM, also is an effective blocker of FAM171A2-α-syn fibril interaction both in vitro and in vivo.

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

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

Bemcentinib (R428, BGB324) is potent, selective and orally bioavailable inhibitor of Axl kinase with IC50 of 14 nM, also is an effective blocker of FAM171A2-α-syn fibril interaction both in vitro and in vivo.
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.