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AMG-337 monohydrate

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names：
1,6-Naphthyridin-5(6H)-one, 6-((1R)-1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo(4,3-a)pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-, hydrate (11)
CAS號(hào)：
1643590-78-6
MDL Number：
MF(分子式)： C23H24FN7O4 MW(分子量)： 481.49
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	AMG-337 monohydrate
英文別名	AMG-337 monohydrate
CAS號(hào)	1643590-78-6
Inchi	1S/C23H22FN7O3.H2O/c1-14(30-5-4-20-18(23(30)32)9-17(11-25-20)34-7-6-33-3)21-27-28-22-19(24)8-15(13-31(21)22)16-10-26-29(2)12-16;/h4-5,8-14H,6-7H2,1-3H3;1H2/t14-;/m1./s1
InchiKey	FQOJZRILDACBLT-PFEQFJNWSA-N
分子式 Formula	C23H24FN7O4
分子量 Molecular Weight	481.49
溶解度Solubility
性狀	Solid powder
儲(chǔ)藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產(chǎn)品說(shuō)明	AMG-337 monohydrate(CAS:1643590-78-6):僅限應(yīng)用于工業(yè)或者科學(xué)研究過(guò)程中非醫(yī)療目的，不應(yīng)用于人類或動(dòng)物的臨床診斷以及治過(guò)程療，該產(chǎn)品非藥用，非食用。
Introduction	AMG-337 monohydrate is a highly selective small molecule MET inhibitor. Aberrant hepatocyte growth factor (HGF)/MET signaling has been implicated in hepatocarcinogenesis, suggesting that MET may serve as an attractive therapeutic target in hepatocellular carcinoma.
Application1
Application2
Application3

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[1]Hong DS, LoRusso P, Hamid O, Janku F, Kittaneh M, Catenacci DVT, Chan E, Bekaii-Saab T, Gadgeel SM, Loberg RD, Amore BM, Hwang YC, Tang R, Ngarmchamnanrith G, Kwak EL. Phase I Study of AMG 337, a Highly Selective Small-molecule MET Inhibitor, in Patients with Advanced Solid Tumors. Clin Cancer Res. 2019 Apr 15;25(8):2403-2413. doi: 10.1158/1078-0432.CCR-18-134[1]Epub 2018 Nov 13. PubMed PMID: 30425090.

[2]Van Cutsem E, Karaszewska B, Kang YK, Chung HC, Shankaran V, Siena S, Go NF, Yang H, Schupp M, Cunningham D. A Multicenter Phase II Study of AMG 337 in Patients with MET-Amplified Gastric/Gastroesophageal Junction/Esophageal Adenocarcinoma and Other MET-Amplified Solid Tumors. Clin Cancer Res. 2019 Apr 15;25(8):2414-2423. doi: 10.1158/1078-0432.CCR-18-1337. Epub 2018 Oct 26. PubMed PMID: 30366938.

[3] Yasui H, Go N, Yang H, Amore BM, Jung AS, Doi T. A Phase 1 study evaluating AMG 337 in Asian patients with advanced solid tumors. Jpn J Clin Oncol. 2017 Aug 1;47(8):772-776. doi: 10.1093/jjco/hyx067. PubMed PMID: 28582510.

[4] Hughes PE, Rex K, Caenepeel S, Yang Y, Zhang Y, Broome MA, Kha HT, Burgess TL, Amore B, Kaplan-Lefko PJ, Moriguchi J, Werner J, Damore MA, Baker D, Choquette DM, Harmange JC, Radinsky R, Kendall R, Dussault I, Coxon A. In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models. Mol Cancer Ther. 2016 Jul;15(7):1568-79. doi: 10.1158/1535-7163.MCT-15-0871. Epub 2016 Apr 19. PubMed PMID: 27196782.

[5] Du Z, Caenepeel S, Shen Y, Rex K, Zhang Y, He Y, Tang ET, Wang O, Zhong W, Zhou H, Huang J, Huang E, Hu L, Coxon A, Zhang M. Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma. Mol Cancer Ther. 2016 Jun;15(6):1227-37. doi: 10.1158/1535-7163.MCT-15-0745. Epub 2016 Mar 29. PubMed PMID: 27196749.

6: Boezio AA, Copeland KW, Rex K, K Albrecht B, Bauer D, Bellon SF, Boezio C, Broome MA, Choquette D, Coxon A, Dussault I, Hirai S, Lewis R, Lin MH, Lohman J, Liu J, Peterson EA, Potashman M, Shimanovich R, Teffera Y, Whittington DA, Vaida KR, Harmange JC. Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-y l)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity. J Med Chem. 2016 Mar 24;59(6):2328-42. doi: 10.1021/acs.jmedchem.5b01716. Epub 2016 Feb 11. PubMed PMID: 26812066.

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