产品说明书

Cabozantinib S-malate

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Chemical Structure| 1140909-48-3 同义名 : 苹果酸卡博替尼 (XL184) ;XL184 S-malate;BMS-907351 S-malate;XL184;Cabozantinib malate
CAS号 : 1140909-48-3
货号 : A212266
分子式 : C32H30FN3O10
纯度 : 99+%
分子量 : 635.593
MDL号 : MFCD20923480
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(165.2 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% propylene glycol+5% Tween 80+65% water 15 mg/mL suspension

生物活性
靶点

  • VEGFR2

    VEGFR2/KDR, IC50:0.035 nM
描述 Cabozantinib S-malate is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.87mL

1.57mL

0.79mL

15.73mL

3.15mL

1.57mL
参考文献

[1]You WK, Sennino B, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res. 2011 Jul 15;71(14):4758-68.

[2]Torres KE, Zhu QS, et al. Activated MET is a molecular prognosticator and potential therapeutic target for malignant peripheral nerve sheath tumors. Clin Cancer Res. 2011 Jun 15;17(12):3943-55.