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JNJ-38877605 纯度: 99.95%
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。
JNJ-38877605 Chemical Structure
CAS No. : 943540-75-8
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥660 | In-stock | |
5 mg | ¥600 | In-stock | |
10 mg | ¥1000 | In-stock | |
50 mg | ¥3000 | In-stock | |
100 mg | ¥5000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
JNJ-38877605 相关产品
•相关化合物库:
- Clinical Compound Library Plus
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- Anti-Cancer Compound Library
- Clinical Compound Library
- Orally Active Compound Library
- Anti-Lung Cancer Compound Library
- Angiogenesis Related Compound Library
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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 statistically significant decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose [3]. |
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Clinical Trial |
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分子量 |
377.35 |
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Formula |
C19H13F2N7 |
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CAS 号 |
943540-75-8 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 30 mg/mL (79.50 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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