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Cabozantinib S-malate
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。
Cabozantinib S-malate图片
CAS NO:1140909-48-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品名称
卡博替尼苹果酸盐
XL184 S-malate
BMS-907351 S-malate
产品介绍
Cabozantinib S-malate (XL184 S-malate) 是一种有效的多受体酪氨酸激酶抑制剂, 抑制VEGFR2c-MetKitAxlFlt3IC50分别为0.035,1.3,4.6,7 和 11.3 nM。
生物活性

Cabozantinib S-malate (XL184 S-malate) is a potent multiplereceptor tyrosine kinasesinhibitor that inhibitsVEGFR2,c-Met,Kit,AxlandFlt3withIC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

IC50& Target

VEGFR2

0.035 nM (IC50)

体外研究
(In Vitro)

Cabozantinib (0.1-0.5μM) inhibits the constitutive and inducible MET phosphorylation and its resultant downstream signaling in all MPNST cells. Cabozantinib (>0.1μM) elicits a significant MPNST cell growth inhibition; higher Cabozantinib doses are needed to inhibit NSC growth. Cabozantinib treatment blocks HGF-induced MPNST motility and invasion (a similar effect of found on NSC)[2]. In cellular assays, 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. Cabozantinib also inhibits tubule formation in response to conditioned media derived from cultures of MDA-MB-231 (IC50=5.1 nM), A431 (IC50=4.1 nM), HT1080 (IC50=7.7 nM), and B16F10 (IC50=4.7 nM) cells[3].

体内研究
(In Vivo)

Cabozantinib (60 mg/kg, i.p.) decreases the tumor vascularity with reductions ranging from 67% at 3 mg/kg to 83% at 30 mg/kg for 7 days in animals. Tumors in RIP-Tag2 mice treated for 7 days beginning at age 10 weeks are 40% smaller after XL880 and 35% smaller after Cabozantinib, compared to corresponding values for vehicle[1]. Cabozantinib (30 mg/kg) significantly decreases the microvessel density in mice[2]. Cabozantinib (100 mg/kg, p.o.) inhibits in vivo stimulation of MET phosphorylation by HGF in liver hepatocytes and VEGF-stimulated phosphorylation of FLK1 with inhibition of both targets sustained through 8 hours postdose. Cabozantinib (100 mg/kg, p.o.) disrupts tumor vasculature and promotes tumor and endothelial cell death. Cabozantinib (1-60 mg/kg, p.o.) inhibits tumor growth and promotes tumor regression in vivo[3].

Clinical Trial
分子量

635.59

性状

Solid

Formula

C32H30FN3O10

CAS 号

1140909-48-3

中文名称

卡博替尼苹果酸盐;苹果酸卡博替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 23 mg/mL(36.19 mM)

H2O :< 0.1 mg/mL(insoluble)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5733 mL7.8667 mL15.7334 mL
5 mM0.3147 mL1.5733 mL3.1467 mL
10 mM0.1573 mL0.7867 mL1.5733 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。