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抑制剂/激活剂

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凋亡与自噬

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Bemcentinib (R428)

Bemcentinib (R428) R428; BGB324

Bemcentinib (R428, BGB324)是一种Axl抑制剂，IC50为14 nM，作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR， EGFR， HER2，和PDGFRβ(高100倍以上)高。

货号：
TK0406
规格：

1mg

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	1037624-75-1
生物活性	Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM.
分子式	C30H34N8
分子量	506.64
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 12.5 mg/mL (24.67 mM; ultrasonic and warming and heat to 60°C)
体内研究	Bemcentinib (R428) (125 mg/kg, p.o.) significantly blocks MDA-MB-231-luc-D3H2LN metastases development in two independent mouse models of breast cancer dissemination, suppresses both tumor angiogenesis and vascular endothelial growth factor (VEGF)-induced corneal neovascularization in vivo. Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) makes mice keep on a high-fat diet resulted in significantly reduced weight gain and subcutaneous and gonadal fat mass.
体外研究	Bemcentinib (R428) (2μM) significantly interferes with mechanisms of migration and invasion of Axlpos melanoma cells at levels comparable to Axl knockdown. Bemcentinib (R428) synergizes with CDDP to enhance suppression of liver micrometastasis. Bemcentinib (R428) (50 nM-1μM) causes a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipid uptake.
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纯度及产品资料	98%

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