JNJ-38877605|943540-75-8|-陌孚医药/Medlife

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JNJ-38877605

目录号: PL05081 纯度: ≥99%

CAS No. :943540-75-8

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中文名称	JNJ-38877605
中文别名	6-[二氟[6-(1-甲基-1H-吡唑-4-基)-1,2,4-三唑并[4,3-b]哒嗪-3-基]甲基]喹啉;6-[二氟[6-(1-甲基-1H-吡唑-4-基)-1,2,4-噻唑并[4,3-b]吡嗪-3-基;6-[二氟[6-(1-甲基-1H-吡唑-4-基)-1,2,4-噻唑并[4,3-B]吡嗪-3-基]甲基]-喹啉;奥当卡替
英文名称	JNJ-38877605
英文别名	6-[Difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline;6-(Difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]-triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline;6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline;J&J Ex-61;Quinoline, 6-[difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]-;JNJ-38877605;JNJ38877605;6-(difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline;JNJ 38877605;15UDG410PN;C19H13F2N7;6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline;Quinoline, 6-(difluoro(6-(1-methy;6-[Difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline (ACI)
Cas No.	943540-75-8
分子式	C₁₉H₁₃F₂N₇
分子量	377.35
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

JNJ-38877605是ATP竞争性c-Met抑制剂，IC50为4 nM，对c-Met的抑制性比对其它200种酪氨酸和丝氨酸-苏氨酸激酶的抑制性要强600倍。

生物活性

JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. IC50 value: 4 nM [1] Target: c-Met in vitro: JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. [1] In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth [2]. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells [3]. in vivo: In mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally with 40 mg/kg/day for 72 hours, results in a statisti

性状

Solid

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]. Perera T, et al. JNJ-38877605: a selective Met kinase inhibitor inducing regression of Met-driven tumor models. Presented at the 99th AACR Annual Meeting; 2008 Apr 12-16
[2]. De Bacco F, et al. Induction of MET by ionizing radiation and its role in radioresistance and invasive growth of cancer. J Natl Cancer Inst. 2011 Apr, 103(8), 645-661.

溶解度数据	In Vitro: DMSO : ≥ 30 mg/mL (79.50 mM)配制储备液

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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。

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