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CAS No.: 913376-84-8

SYN1143 Catalog No. CSN25585

Synonyms: c-Met/RON Dual Kinase Inhibitor;RON-IN-1;AMG-1

c-Met/RON Dual Kinase Inhibitor is a potent inhibitor against the kinase activities of HGF receptor c-Met and MSP (Macrophage Stimulating Protein) receptor RON with IC50 of 4 and 9 nM, respectively, and it is reported to inhibit NIH3T3 TRP-Met and U-87 tumor growth in mice in vivo in a dose-dependent manner.

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技术信息

生物活性

描述Recepteur d'origine nantais (RON) and c-Met are receptor tyrosine kinases involved in cell proliferation, migration, and invasion, all of which are key biological events in tumorigenesis. RON-IN-1 is a potent inhibitor of both RON and c-Met that selectively inhibited their kinase activities with IC50 values of 9nM and 4nM, respectively. It shows weak inhibitory activity towards Lck, Tie2, Src, and BTK with IC50 values ranging from 160 to 710nM. In HT-29 and BxPC3 cells, RON-IN-1 at 10 – 1000nM inhibited hepatocyte growth factor-mediated c-Met phosphorylation and downstream signaling in a dose-dependent manner. RON-IN-1 at 10 – 1000nM also inhibited NIH3T3 TPR-Met cell migration. In NIH3T3 RON and BxPC3 cells, treatment with RON-IN-1 (10 – 1000nM) dose-dependently inhibited RON signaling and functional activity. Treatment of NIH3T3 TPR-Met tumor-bearing mice with RON-IN-1 (30 or 100mg/kg once daily, or 30mg/kg twice daily) significantly inhibited tumor growth compared with vehicle-treated control animals. RON-IN-1 (30 or 100mg/kg once daily) also significantly and dose-dependently reduced tumor growth in mice bearing established HT-29 tumors^[1].
参考文献

[1] Zhang Y, Kaplan-Lefko PJ, Rex K, Yang Y, Moriguchi J, Osgood T, Mattson B, Coxon A, Reese M, Kim TS, Lin J, Chen A, Burgess TL, Dussault I. Identification of a novel recepteur d'origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 2008 Aug 15;68(16):6680-7.

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
- 1.7967 mL
- 8.9834 mL
- 17.9667 mL
- 5 mM
- 0.3593 mL
- 1.7967 mL
- 3.5933 mL
- 10 mM
- 0.1797 mL
- 0.8983 mL
- 1.7967 mL

技术信息

CAS号

913376-84-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H29FN4O5

运输

蓝冰

分子量

556.58

别名

c-Met/RON Dual Kinase Inhibitor;RON-IN-1;AMG-1;RON inhibitor-1;Ron Inhibitor I;Met Kinase Inhbitor IV

溶解度

DMSO	100.0 mg/mL (179.7 mM)
Water	Insoluble
Ethanol	60.0 mg/mL (107.8 mM)

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