卡博替尼.|849217-68-1|(卡博替尼; XL184; BMS-907351)-陌孚医药/Medlife

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

目录号: PC10002 纯度: >99%

CAS No. :849217-68-1

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中文名称	卡博替尼.
中文别名	卡博替尼;卡博替尼;Cabozantinib (XL184, BMS-907351) 抑制剂;Cabozantinib标准品;N-(4-(6,7-二甲氧基喹啉-4-基氧基)苯基)-N-(4-氟苯基)环丙烷-1,1-二羧酰胺;XL184（博卡替尼）;XL184（卡博替尼）靶向药;XL184（卡博替尼）粉末;XL184（卡博替尼）固体状;XL184,卡博替尼;卡巴唑替尼;卡博替尼 XL184;卡博替尼 cabozantinib;卡博替尼（CABOZANTINIB）;卡博替尼苹果酸盐;卡博替尼中间体;科研实验XL184（卡博替尼）;临床实验XL184;苹果酸盐;苹果酸盐Cabozantinib,XL-184;医药级XL184（卡博替尼）;N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基]-N'-(4-氟苯基)-1,1-环丙烷二甲酰胺;博卡替尼;卡赞替尼;苹果酸盐CABOZANTINIB杀菌原材料;苹果酸盐CABXL-184;鑫源顺卡博替尼;卡波替尼杂质
英文名称	Cabozantinib
英文别名	XL184;Cabozantinib (XL184, BMS-907351);1,1-Cyclopropanedicarboxamide,N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-;1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;C28H24FN3O5;Cabozantinib;Cabozantinib (XL184,BMS 907351,Cometriq®);Cabozantinib S-malate;Cabozantinib, XL184;N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;XL-180;XL-184;XL184 Cabozantinib;[14C]-Cabozantinib;BMS907351;BMS-907351;Cometriq;cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinoline-4-yloxy)-phenyl]-amide (4-fluoro-phenyl)-amide;N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide;Cabozantinib Impurity
Cas No.	849217-68-1
分子式	C₂₈H₂₄FN₃O₅
分子量	501.51
包装储存	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.

性状

Solid

IC50 & Target[1][2]

VEGFR2

0.035 nM (IC₅₀)

Flt-4

6 nM (IC₅₀)

Flt-1

12 nM (IC₅₀)

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.
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.
Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion.
Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types.

Medlife 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
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.

Cell Migration Assay

Cell Line:	B16F10 cells
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
Concentration:	0, 1.5, 14, and 123 nM
Incubation Time:	24 hours
Result:	Potently inhibited HGF-induced invasion (IC₅₀ = 9 nM) of B16F10 cells.

体内研究(In Vivo)

Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice.
Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis.
Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner.

Medlife 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)
Dosage:	0, 100 mg/kg
Administration:	Orally, once
Result:	Inhibited MET and VEGFR2 phosphorylation.

Animal Model:	Mice bearing MBA-MB-231 tumor
Dosage:	1, 3, 10, 30, 60 mg/kg
Administration:	Orally, once daily for 14 days
Result:	Inhibited tumor growth in a dose-dependent manner.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

参考文献

[1]. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308. [Information]

[2]. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768. [Information]

[3]. Fuse MA, et al. Combination Therapy With c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. Mol Cancer Ther. Mol Cancer Ther. 2017 Nov;16(11):2387-2398. [Information]

溶解度数据

体外研究:

DMSO : 25 mg/mL (49.85 mM; Need ultrasonic)

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 30% polypropylene glycol, 5% Tween-80 and 65% D5W (dextrose 5% water)
Solubility: 10 mg/mL (19.94 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 0.5% CMC/saline water
Solubility: 2.5 mg/mL (4.98 mM); Suspended solution; Need ultrasonic
3.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.98 mM); Clear solution
4.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
5.

建议依照次序添加每种溶剂： 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
6.

建议依照次序添加每种溶剂： 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。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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