Cabozantinib - CAS:849217-68-1

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Cabozantinib (Synonyms:卡博替尼; XL184; BMS-907351)

目录号 : KM5258 CAS No. : 849217-68-1 纯度 : 98%

Data Sheet 产品使用指南

Cabozantinib是一种有效的多受体酪氨酸激酶抑制剂，抑制VEGFR2，c-Met，Kit，Axl 和 Flt3 的 IC₅₀ 分别为0.035，1.3，4.6，7 和 11.3 nM。

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10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg		In-stock
500mg	询价	In-stock
1g	询价	In-stock

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生物活性

Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC₅₀s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

体外研究

Cabozantinib is a potent inhibitor of MET and VEGFR2 with IC₅₀ values of 1.3 and 0.035 nM, respectively. MET-activating kinase domain mutations Y1248H, D1246N, or K1262R are also inhibited by Cabozantinib (IC₅₀=3.8, 11.8, and 14.6 nM, respectively). Cabozantinib displays strong inhibition of several kinases that have also been implicated in tumor pathobiology, including KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). In cellular assays, 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. The effect of Cabozantinib on proliferation is evaluated in a number of human tumor cell lines. SNU-5 and Hs746T cells harboring amplified MET are the most sensitive to Cabozantinib (IC₅₀=19 and 9.9 nM, respectively); however, SNU-1 and SNU-16 cells lacking MET amplification are more resistant (IC₅₀=5,223 and 1,149 nM, respectively). MDA-MB-231 and U87MG cells exhibit comparable levels of sensitivity to Cabozantinib (IC₅₀=6,421 and 1,851 nM, respectively), whereas H441, H69, and PC3 cell lines are the least sensitive to Cabozantinib with IC₅₀ values of 21,700, 20,200, and 10,800 nM, respectively. In addition, BaF3 cells expressing human FLT3-ITD, an activating mutation in acute myelogenous leukemia, are sensitive to Cabozantinib (IC₅₀=15 nM) when compared with wild-type BaF3 cells (IC₅₀=9,641 nM).

体内研究

Tumor vascularity decreases after Cabozantinib (XL184), with reductions ranging from 67% at 3 mg/kg to 83% at 30 mg/kg for 7 days. In mouse models, Cabozantinib dramatically alters tumor pathology, resulting in decreased tumor and endothelial cell proliferation coupled with increased apoptosis and dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models. Importantly, treatment with Cabozantinib does not increase lung tumor burden in an experimental model of metastasis, which has been observed with inhibitors of VEGF signaling that do not target MET. On a body weight dosage basis, Cabozantinib plasma exposures range from 6- to 10-fold higher in rats than in mice, which accounts for lower doses inducing tumor growth inhibition/regression in rats than in mice. Subchronic administration of Cabozantinib is well tolerated in mice and rats with no signs of toxicity, as determined by stable and/or increasing body weights during the treatment period.

分子式

C₂₈H₂₄FN₃O₅

分子量

501.51

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.

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 : ≥ 30 mg/mL (59.82 mM)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* "≥" means soluble, but saturation unknown.

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：

——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-80 and 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-CD in 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-CD in 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 μL 20% 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。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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KKL 顾客使用本产品发表的 26 篇科研文献

The molarity calculator equation

The dilution calculator equation