Bemcentinib (Synonyms:R428; BGB324)
目录号 : KM5627 CAS No. : 1037624-75-1 纯度 : 98%

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

规格 价格 是否有货 数量
2mg
In-stock
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM.

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.

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.

分子式
C30H34N8
分子量
506.64
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 : 12.5 mg/mL (24.67 mM; ultrasonic and warming and heat to 60°C)

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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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% Tween-80 in Saline water

    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-CD in 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 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均 匀。

     
临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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