生物活性
Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis
体外研究
(In Vitro)
Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively[1].
Cabozantinib (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively[1].
Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion[1].
Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
Cell Line: SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells[1]
Concentration:
Incubation Time: 48 hours
Result: Inhibited tumor cell proliferation, with IC50 of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively.
体内研究
(In Vivo)
Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice[1].
Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis[1].
Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Female mice bearing MBA-MB-231 tumor (5 per group)[1]
Dosage: 0, 100 mg/kg
Administration: Orally, once
Result: Inhibited MET and VEGFR2 phosphorylation.
分子量
501.51
性状
Solid
Formula
C28H24FN3O5
CAS 号
849217-68-1
中文名称
卡博替尼
运输条件
Room temperature in continental US; may vary elsewhere.
溶解性数据
In Vitro:
DMSO : 25 mg/mL (49.85 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 1.9940 mL 9.9699 mL 19.9398 mL
5 mM 0.3988 mL 1.9940 mL 3.9880 mL
10 mM 0.1994 mL 0.9970 mL 1.9940 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 (protect from light)。-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: