货号	规格	价格	上海	北京	珠海	重庆	武汉
S81087-2mg买3赠1	99.70%	￥200.00 S81087-2mg ￥200.00 现货（买3赠1）	9 9	-	-	-	-
S81087-5mg买3赠1	99.70%	￥352.00 S81087-5mg ￥352.00 现货（买3赠1）	8 8	-	-	-	-
S81087-10mg买3赠1	99.70%	￥472.00 S81087-10mg ￥472.00 现货（买3赠1）	7 7	-	-	-	-
S81087-50mg买3赠1	99.70%	￥1200.00 S81087-50mg ￥1200.00 现货（买3赠1）	6 6	-	-	-	-
S81087-100mg买3赠1	≥99%	￥2240.00 S81087-100mg ￥2240.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S81087-200mg买3赠1	≥99%	￥4320.00 S81087-200mg ￥4320.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

Tivantinib is a highly selective c-Met tyrosine kinase inhibitor with a Ki of 355 nM.

靶点：

Ki: 355 nM (c-Met);Apoptosis; c-Met/HGFR

体内研究：

Pharmacodynamically, the phosphorylation of c-Met in human colon xenograft tumors (HT29) is strongly inhibited by Tivantinib (ARQ 197), as assessed by a dramatic reduction of c-Met autophosphorylation 24 hours after a single oral dose of 200 mg/kg of Tivantinib. This same dosage in mice shows that tumor xenografts are exposed to sustained plasma levels of Tivantinib, consistent with the observed pharmacodynamic inhibition of c-Met phosphorylation and inhibition of proliferation of c-Met harboring cancer cell lines. A Cmax of 5.73 μg/mL (13 μM), an area under the concentration-time curve of 12.1 μg/mL h, and a t1/2 of 2.4 hours are measured. Plasma levels of Tivantinib 10 hours after dosing are determined to be 1.3 μM, >3-fold above the biochemical inhibitory constant of Tivantinib for c-Met

参考文献：

1. Munshi N, et al. ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity. Mol Cancer Ther. 2010 Jun;9(6):1544-53. 2. Bai YL, et al. Quantitative analysis of tivantinib in rat plasma using ultra performance liquid chromatography with tandem mass spectrometry. J Pharm Biomed Anal. 2016 Jul 15;126:98-102.

溶解性：

DMSO : 100 mg/mL (270.69 mM; Need ultrasonic)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.707 ml	13.535 ml	27.069 ml
5 mM	0.541 ml	2.707 ml	5.414 ml
10 mM	0.271 ml	1.353 ml	2.707 ml
50 mM	0.054 ml	0.271 ml	0.541 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献(1篇)

1. [IF=5.988] Wen Jiang et al."Rapid Determination of 9 Tyrosine Kinase Inhibitors for the Treatment of Hepatocellular Carcinoma in Human Plasma by QuEChERS-UPLC-MS/MS."Frontiers in Pharmacology.2022; 13: 920436

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