JNJ-38877605

An inhibitor of Met kinase

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库存: 现货

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5mg

￥412.00

330.00

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25mg

￥1962.00

1570.00

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100mg

￥5400.00

4320.00

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货号: ajci9412
CAS: 943540-75-8
别名: 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
分子式: C19H13F2N7
分子量: 377.35
纯度: >98%
溶解度: ≥ 18.85mg/mL in DMSO, ≥ 3.25 mg/mL in EtOH with ultrasonic
储存: Store at -20°C
库存: 现货

Background

JNJ-38877605 is a small-molecule ATP-competitive inhibitor of the catalytic activity of c-Met.

Extensive evidence that c-Met signaling is involved in the progression and spread of several cancers and an enhanced understanding of its role in disease have generated considerable interest in c-Met and HGF asmajor targets in anti-cancer drug development.

In vitro: JNJ-38877605 showed ~600-fold selectivity for c-Met compared with a panel of ~250 diverse tyrosine and serine-threonine kinases and was found to potently inhibit HGF-stimulated and constitutively activated c-Met phosphorylation in vitro [1].

In vivo: JNJ-38877605 showed excellent oral bioavailability approaching 100% in all examined species. In addition, JNJ-38877605 in a single dose was observed toinhibit Met phosphorylation in tumor xenografts for up to16 h. Inhibition of Met phosphorylation was associated withdose-dependent tumor growth inhibition using a range of oral dosing regimens [2].

Clinical trial: A Safety and Dose-finding Study of JNJ-38877605 in Patients With Advanced or Refractory Solid Tumors.

Reference:
[1] PereraT, L avrijssenT, Janssens B, 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;