Capmatinib|1029712-80-8|(卡马替尼; INC280; INCB28060)-陌孚医药/Medlife

您当前的位置：

Capmatinib (Synonyms: 卡马替尼; INC280; INCB28060)

目录号: PL03389 纯度: ≥99%

CAS No. :1029712-80-8

商品编号	规格	价格	会员价
PL03389-5mg	5mg	¥976.73	请登录
PL03389-10mg	10mg	¥1174.55	请登录
PL03389-50mg	50mg	¥3832.73	请登录
PL03389-100mg	100mg	¥6800.00	请登录
PL03389-200mg	200mg	¥9520.00	请登录
PL03389-500mg	500mg	询价	询价
PL03389-1g	1g	询价	询价
PL03389-10mM*1mLinDMSO	10mM*1mLinDMSO	¥1074.40	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称	Capmatinib
中文别名	苯扎米特;2-氟-N-甲基-4-[7-[(喹啉-6-基)甲基]咪唑并[1,2-B]-[1,2,4]三嗪-2-基]苯甲酰胺;Capmatinib (INCB28060) 抑制剂;INCB28060 苯扎米特;INCB28060(苯扎米特);苯扎米特 INCB28060;苯扎米特固体状;苯扎米特中间体;科研实验苯扎米特;临床实验苯扎米特;INCB28060;卡马替尼
英文名称	Capmatinib
英文别名	INCB28060;1 week;2-Fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide;2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide;Capmatinib;Capmatinib (INCB28060);inc280;INCB28060(Capmatinib);BenzaMide;INCB280;2-fluoro-N-methyl-4-[(7-quinolin-6-ylmethyl)imidazo[1,2-b]triazin-2-yl]benzamide;2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide;2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazolo[1,2-b][1,2,4]triazin-2-yl]benzamide;INC-280;INCB-28060;QC-7530;UNII-TY34L4F9OZ;NC280;INC28060;INCB028060;NVP-INC280;BenzaMide HCl;INCB28060, INC280;INC 280 (INCB28060);TY34L4F9OZ;INCB 28060;2-Fluoro-N-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]triazin-2-yl]benzamide;BenzaMide, 2-fluoro-N-Methyl-4-[7-(6-quinolinylMethyl)iMidazo[1,2-b][1,2,4]triazin-2-yl]-;C2;Tabrecta;2-Fluoro-N-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]tr
Cas No.	1029712-80-8
分子式	C₂₃H₁₇FN₆O
分子量	412.42
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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 (IC 50 =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.

性状

Solid

IC50 & Target[1][2]

IC50: 0.13 nM (c-MET)

体外研究(In Vitro)

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

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

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

ClinicalTrial

参考文献

[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.
[2]. 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.

溶解度数据	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

搜索质检报告(COA)

产品使用指南

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。

相关产品

The molarity calculator equation

The dilution calculator equation