AMG-337|1173699-31-4|-陌孚医药/Medlife

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AMG-337

目录号: PL04826 纯度: ≥99%

CAS No. :1173699-31-4

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中文名称	AMG-337
中文别名	6-[(1R)-1-[8-氟-6-(1-甲基-1H-吡唑-4-基)-1,2,4-三唑并[4,3-a]吡啶-3-基]乙基]-3-(2-甲氧基乙氧基)-1,6-萘啶-5(6H)-酮;AMG-337
英文名称	AMG-337
英文别名	AMG-337;Compound M;(R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one;AMG337;AMG 337;08WG8S0L8D;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)-;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)-;AMG 337 [WHO-DD];BCP16602;s8167;BDBM50157612;SB19194;A16400
Cas No.	1173699-31-4
分子式	C₂₃H₂₂FN₇O₃
分子量	463.46
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

AMG-337 是一种口服有效的选择性 MET 激酶抑制剂，抑制 WT MET、H1094R MET、M1250T MET、HGF-stimulated pMET (PC3 细胞) MET、V1092I MET、Y1230H MET 和 D1228H MET 的 IC₅₀ 值分别为 1、1、4.7、5、21.5、1077 和 >4000 nM。AMG 337 在 MET 扩增的癌细胞系中抑制 MET 及其下游效应子的磷酸化，从而抑制 MET 依赖的细胞增殖和诱导凋亡

生物活性

AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC 50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.

性状

Solid

IC50 & Target[1][2]

IC50: 1 (WT MET), 1 (H1094R MET), 4.7 (M1250T MET), 5 (HGF-stimulated pMET (PC3 cells) MET), 21.5 (V1092I MET), 1077 (Y1230H MET) and >4000 nM (D1228H MET)

体外研究(In Vitro)

AMG 337 (0-3 μM; 72 h) inhibits proliferation in MET-dependent cancer cell lines.
AMG 337 (0-300 nM; 0-24 h; MKN-45, SNU-620, and SNU-5 cells) inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis. has not independently confirmed the accuracy of these methods. They are for reference only.Apoptosis Analysis

体内研究(In Vivo)

AMG 337 (0-30 mg/kg; p.o.; daily, for 28 d) inhibits MET signaling in tumor xenografts and inhibits tumor growth in MET-dependent tumor xenograft models.
AMG 337 (0-3 mg/kg; p.o.; once, for 3 or 24 h) is associated with increased necrosis in the MET-dependent SNU-620 tumor xenograft 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]. Hughes PE, et, al. 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.
[2]. Du Z, et, al. Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma. Mol Cancer Ther. 2016 Jun;15(6):1227-37.

溶解度数据	In Vitro: DMSO : 100 mg/mL (215.77 mM; Need ultrasonic)配制储备液

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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。

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