生物活性 | Cabozantinib is a potent and orally active inhibitor ofVEGFR2andMET, withIC50values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition ofKIT,RET,AXL,TIE2, andFLT3(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 cellapoptosis[1][2]. |
IC50& Target[1] | VEGFR2 0.035 nM (IC50) | Flt-4 6 nM (IC50) | Flt-1 12 nM (IC50) |
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体外研究 (In Vitro) | Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50values 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 IC50values 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].
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 IC50of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively. |
Cell Migration Assay Cell Line: | B16F10 cells[1] | Concentration: | 0, 41, 123, and 370 nM | Incubation Time: | 24 hours | Result: | Potently inhibited HGF-induced migration (IC50= 31 nM) of B16F10 cells. |
Cell Invasion Assay Cell Line: | B16F10 cells[1] | Concentration: | 0, 1.5, 14, and 123 nM | Incubation Time: | 24 hours | Result: | Potently inhibited HGF-induced invasion (IC50= 9 nM) of B16F10 cells. |
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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].
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. |
Animal Model: | Mice bearing MBA-MB-231 tumor[1] | Dosage: | 1, 3, 10, 30, 60 mg/kg | Administration: | Orally, once daily for 14 days | Result: | Inhibited tumor growth in a dose-dependent manner. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
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℃)(insoluble) 配制储备液 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℃, 6 months; -20℃, 1 month (protect from light)。-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: 30% polypropylene glycol, 5%Tween-80and 65% D5W (dextrose 5% water) Solubility: 10 mg/mL (19.94 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂: 0.5% CMC/saline water Solubility: 2.5 mg/mL (4.98 mM); Suspended solution; Need ultrasonic 3. 请依序添加每种溶剂: 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.98 mM); Clear solution 4. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.15 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 5. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (4.15 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.15 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。 6. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.15 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 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玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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