Capmatinib 卡马替尼; INC280; INCB28060|cas:1029712-80-8|西域试剂

Capmatinib 卡马替尼; INC280; INCB28060,99.92%

产品编号：Bellancom-13404| CAS NO：1029712-80-8| 分子式：C₂₃H₁₇FN₆O| 分子量：412.42

Capmatinib (INCB28060) 是一种有效的选择性c-MET 激酶抑制剂。Capmatinib (INCB28060) 抑制 c-MET 激酶活性，平均IC50 为 0.13 nM。

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货号	价格	库存与货期
Bellancom-13404	￥790.00	杭州北京（现货）
Bellancom-13404	￥950.00	杭州北京（现货）
Bellancom-13404	￥3100.00	杭州北京（现货）
Bellancom-13404	￥5500.00	杭州北京（现货）
Bellancom-13404	￥7700.00	杭州北京（现货）

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Capmatinib 卡马替尼; INC280; INCB28060

产品介绍

Capmatinib (INC280; INCB28060) 是一种有效的、口服活性的、选择性的、ATP 竞争性的 c-Met 激酶抑制剂 (IC₅₀=0.13 nM)。Capmatinib 可抑制 c-MET 的磷酸化，以及 c-MET 通路下游效应蛋白如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。Capmatinib 有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移，并有效诱导细胞凋亡。在肿瘤小鼠模型中表现出抗肿瘤活性。Capmatinib 主要由 CYP3A4 和醛氧化酶代谢。

生物活性

Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase.

体外研究

Capmatinib (INCB28060) inhibits c-MET phosphorylation with an IC₅₀ value of approximately 1 nM and a concentration of approximately 4 nM inhibits c-MET more than 90%, which is reversible and the effect is significantly reduced in several hours after the compound is removed and completely disappeared by 48 hours.
Capmatinib (INCB28060) (0-10000 nM; 72 h) inhibits the proliferation of SNU-5, S114, H441 and U-87MG.
Capmatinib (INCB28060) (0.06-62.25 nM; 2h) effectively inhibits phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5.
Capmatinib (INCB28060) (0.24-63 nM; over night) prevents HGF-stimulated H441 cell migration.
Capmatinib (INCB28060) (0.5-50 nM; 20 min) suppresses phosphorylation of both EGFR and HER-3 rapidly.
Capmatinib (INCB28060) (0-333 nM; 24 h) induces apoptosis in SNU-5 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	SNU-5, S114, H441 and U-87MG
Concentration:	0-10000 nM
Incubation Time:	72 h
Result:	Inhibited the cell viability of SNU-5 and S114, as well as the colony formation of H441 and U-87MG, with IC₅₀ values of 1.2 nM, 12.4 nM, ~0.5 nM and 2 nM, respectively.

Cell Migration Assay

Cell Line:	H441 (stimulated with 50 ng/mL recombinant human HGF for 24h)
Concentration:	0.24, 1, 4, 16 and 63 nM
Incubation Time:	Over night
Result:	Prevented HGF-stimulated H441 cell migration, with IC₅₀ of approximately 2 nM, and less cell migration at 16 nM.

Western Blot Analysis

Cell Line:	SNU-5
Concentration:	0.06, 0.24, 0.98, 3.91, 15.63 and 62.25 nM
Incubation Time:	2 h
Result:	Effectively inhibited phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5.

Western Blot Analysis

Cell Line:	H1993 cells
Concentration:	0.5, 5 and 50 nM
Incubation Time:	20 min
Result:	Suppressed phosphorylation of both EGFR and HER-3 rapidly and as effectively as the compound inhibited c-MET phosphorylation in H1993 cells.

Apoptosis Analysis

Cell Line:	SNU-5 cells
Concentration:	0.017, 0.15, 1.37, 12.33, 111 and 333 nM
Incubation Time:	24 h
Result:	Effectively induced DNA fragmentation.

体内研究
(In Vivo)

Capmatinib (INCB28060) (1-30 mg/kg; PO, twice daily, for 2 weeks) exhibits dose-dependent inhibition of tumor growth, and shows well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss in U-87MG tumor mice model.
Capmatinib (INCB28060) (0.03-10 mg/kg; PO, single dosage) causes inhibition of c-MET phosphorylation in S114 tumor mice model.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c nu/nu mice (inoculated subcutaneously with 5×10⁶ U-87MG glioblastoma cells)
Dosage:	1, 3, 10 and 30 mg/kg
Administration:	PO, twice daily, for 2 weeks
Result:	Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.

Animal Model:	Female Balb/c nu/nu mice (inoculated subcutaneously with 4×10⁶ S114 tumor cells)
Dosage:	0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
Administration:	PO, single dosage
Result:	Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c nu/nu mice (inoculated subcutaneously with 5×10⁶ U-87MG glioblastoma cells)
Dosage:	1, 3, 10 and 30 mg/kg
Administration:	PO, twice daily, for 2 weeks
Result:	Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.

Animal Model:	Female Balb/c nu/nu mice (inoculated subcutaneously with 4×10⁶ S114 tumor cells)
Dosage:	0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
Administration:	PO, single dosage
Result:	Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c nu/nu mice (inoculated subcutaneously with 5×10⁶ U-87MG glioblastoma cells)
Dosage:	1, 3, 10 and 30 mg/kg
Administration:	PO, twice daily, for 2 weeks
Result:	Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.

Animal Model:	Female Balb/c nu/nu mice (inoculated subcutaneously with 4×10⁶ S114 tumor cells)
Dosage:	0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
Administration:	PO, single dosage
Result:	Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (60.62 mM; Need ultrasonic)

H₂O : 4 mg/mL (9.70 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4247 mL	12.1236 mL	24.2471 mL
5 mM	0.4849 mL	2.4247 mL	4.8494 mL
10 mM	0.2425 mL	1.2124 mL	2.4247 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。-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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.04 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 ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.04 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 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

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38. [Content Brief]

. Baltschukat S, et al. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation. Clin Cancer Res. 2019 May 15;25(10):3164-3175. [Content Brief]

. Dhillon S. Capmatinib: First Approval. Drugs. 2020 Jul;80(11):1125-1131. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	Capmatinib (INCB28060)
CAS号：	1029712-80-8
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Capmatinib (INCB28060)
别名：	INC280; Capmatinib; NVP-INC280
分子式：	C23H17FN6O
分子量：	412.42

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

1029714-88-2

74-89-5

~84%

1029712-80-8

文献：Weng, Lingkai; Qiao, Lei; Zhou, Jiacheng; Liu, Pingli; Pan, Yongchun Patent: US2009/291956 A1, 2009 ; Location in patent: Page/Page column 24-25 ;

上游产品 1
74-89-5
下游产品 0

[1]. Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38.

Capmatinib 卡马替尼; INC280; INCB28060,99.92%

Capmatinib 卡马替尼; INC280; INCB28060

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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