Bemcentinib

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Bemcentinib

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1037624-75-1

R428
BGB324

Bemcentinib (R428) 是一种高效的具有选择性的Axl抑制剂，IC₅₀值为 14 nM。

生物活性

Bemcentinib (R428) is a potent and selective inhibitor ofAxlwith anIC₅₀of 14 nM^[2].

IC₅₀& Target

IC50: 14 nM (Axl kinase)

体外研究
(In Vitro)

Bemcentinib (R428) (2μM) significantly interferes with mechanisms of migration and invasion of Axlpos melanoma cells at levels comparable to Axl knockdown^[1]. Bemcentinib (R428) synergizes with CDDP to enhance suppression of liver micrometastasis^[2]. Bemcentinib (R428) (50 nM-1μM) causes a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipid uptake^[3].

体内研究
(In Vivo)

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^[2]. 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^[3].

Clinical Trial

分子量

506.64

性状

Solid

Formula

C₃₀H₃₄N₈

CAS 号

1037624-75-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL(49.34 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.9738 mL	9.8689 mL	19.7379 mL
5 mM	0.3948 mL	1.9738 mL	3.9476 mL
10 mM	0.1974 mL	0.9869 mL	1.9738 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 0.5%CMC-Na/saline water
Solubility: 12.5 mg/mL (24.67 mM); Suspended solution; Need ultrasonic
2.
请依序添加每种溶剂： 0.5%HPMC 1%Tween80
Solubility: 5 mg/mL (9.87 mM); Suspended solution; Need ultrasonic
3.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline)
Solubility: 2.08 mg/mL (4.11 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.11 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在本网站选购。