|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|CsnPharm

CAS No.: 1029712-80-8

Capmatinib/卡马替尼 Catalog No. CSN15776

Synonyms: INC280;INCB28060;NVP INC-280

INCB28060 is a potent and selective c-MET kinase inhibitor. INCB28060 inhibits c-MET kinase activity with an average IC50 of 0.13 nM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 c-Met

IC50:0.13nM
描述The overexpression and activation of the Met receptor and its ligand HGF (hepatocyte growth factor) are associated with a wide variety of human malignancies, as well as the tumor invasion. Capmatinib is a highly selective and potent c-Met inhibitor with IC50 values of 0.13nM (measured by recombinant kinase assays), without direct inhibitory effect on the RONβ, EGFR and HER-3. Cellular study showed a dose-dependent inhibition by Capmatinib against c-MET activation in both cells with constitutively active c-MET, such as SNU-5 (IC50=1.1nM) and S114 (IC50=0.9nM), and cells with HGF-stimulated c-MET, like A549 (IC50=0.7nM), U-87MG (IC50=1nM), 786-0 (IC50=0.6nM), H441 (IC50=0.7nM), H596 (IC50=0.4nM) and H1437 (IC50=0.3nM). Treatment with Capmatinib for 2h at concentration>0.98nM caused significant decreased p-c-MET, and its major downstream effectors, including phosphorylation of ERK1/2 (≥3.91nM), AKT (>0.98nM), FAK (≥3.91nM), GAB1(≥3.91nM), STAT3 (≥0.24nM)/5 (≥0.98nM), in SNU-5 with constitutively active c-MET. Consistent with this, Capmatinib suppressed growth of SNU-5 cells, with IC50 value of 1.2nM and a calculated IC90 value of 4.6nM, in c-Met-dependent manner. Significant apoptosis can be observed in SNU-5 cells treated with Capmatinib at concentration>5nM through DNA fragmentation and cleaved PARP. As prediction, Capmatinib dose-dependently prevented anchorage-independent U-87MG cell growth in soft agar and HGF-stimulated H441 cell migration at concentration ranging in 1-63nM. Though Capmatinib did not directly inhibit the other RTKs in kinase assays, the suppression of p-EGFR and p-HER3 by Capmatinib through cross talk in H1993 cells. Oral administration of Capmatinib at dose of 3, 10 and 30mg/kg for 2 weeks caused tumor growth inhibition dose-dependently in both mice xenograft S114 and U-87MG, with significant c-MET-phosphorylation in vivo^[1].
作用机制Capmatinib is an ATP-competitive c-MET inhibitor.^[1]
动物研究
剂量
Mice: 1 mg/kg - 30 mg/kg^[1] (p.o.), 44 mg/kg^[2] (p.o.)

给药途径
p.o.

动物研究
剂量	Mice: 1 mg/kg - 30 mg/kg^[1] (p.o.), 44 mg/kg^[2] (p.o.)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4247 mL
- 12.1236 mL
- 24.2472 mL
- 5 mM
- 0.4849 mL
- 2.4247 mL
- 4.8494 mL
- 10 mM
- 0.2425 mL
- 1.2124 mL
- 2.4247 mL

技术信息

CAS号

1029712-80-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H17FN6O

运输

蓝冰

分子量

412.42

别名

INC280;INCB28060;NVP INC-280;INCB-028060;卡马替尼

溶解度

DMSO	2.0 mg/mL (4.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Capmatinib/卡马替尼 Catalog No. CSN15776

靶点选择性

请登录您的专属账户

确认信息