MK-5108|1010085-13-8|(VX-689)-陌孚医药/Medlife

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MK-5108 (Synonyms: VX-689)

目录号: PL13939 纯度: ≥99%

CAS No. :1010085-13-8

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PL13939-200mg	200mg	询价	询价
PL13939-500mg	500mg	询价	询价
PL13939-10mM*1mLinDMSO	10mM*1mLinDMSO	¥1639.00	请登录

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中文名称	MK-5108
中文别名	MK-5108 (VX-689) 抑制剂;反式-4-(3-氯-2-氟苯氧基)-1-[[6-(2-噻唑基氨基)-2-吡啶基]甲基]环己烷甲酸
英文名称	MK-5108
英文别名	MK-5198;(1r,4r)-4-(3-chloro-2-fluorophenoxy)-1-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)cyclohexanecarboxylic acid;MK-5108 (VX-689);4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)pyridin-2-yl]methyl]cyclohexane-1-carboxylic acid;MK 5108;MK-5108;VX689;BCP9000941;cc-619;UNII-H8J407531S;VX-689;trans-4-(3-Chloro-2-fluorophenoxy)-1-{[6-(1,3-thiazol-2-ylamino)-2-pyridinyl]methyl}cyclohexanecarboxylic acid;trans-4-(3-Chloro-2-fluorophenoxy)-1-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]cyclohexanecarboxylic acid;MK5108;VX 689;H8J407531S;(1r,4r)-4-(3-chloro-2-fluorophenoxy)-1-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)cyclohexane-1-carboxylic acid;4-(3-Chloranyl-2-Fluoranyl-Phenoxy)-1-[[6-(1,3-Thiazol-2-Ylamino)pyridin-2-Yl]methyl]cyclohexane-1-Carboxylic Acid;Cyclohexanecarboxylic acid, 4-(3-chloro-2-fluorophe
Cas No.	1010085-13-8
分子式	C₂₂H₂₁ClFN₃O₃S
分子量	461.94
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

MK-5108是高效和特异性的极光激酶A抑制剂，IC₅₀ 值为0.064 nM。

生物活性

MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC 50 value of 0.064 nM.

性状

Solid

IC50 & Target[1][2]

Aurora A 64 pM (IC50)

体外研究(In Vitro)

MK-5108 inhibits Aurora-A activity with an IC50 value of 0.064 nM in an ATP-competitive manner. It shows robust selectivity against the other family kinases Aurora-B (220-fold) and Aurora-C (190-fold). MK-5108 also exhibits high selectivity for Aurora-A over other protein kinases. MK-5108 inhibits the growth of 14 cell lines with IC50 values between 0.16 and 6.4 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

MK-5108 treatments at 15 and 30 mg/kg results in significant tumor growth inhibition in the HCT116 tumor model. MK-5108 is well tolerated at both doses, with minimal reduction in body weight. MK-5108 also exhibits significant antitumor activity in nude rats bearing SW48 tumors. MK-5108 at 15 and 45 mg/kg causes dose-dependent tumor growth inhibition with a %T/C of 35% and 7% at day 10, and 58% and 32% at day 27, respectively. MK-5108 is well tolerated in nude rats, with no body weight reduction and moderate effect on blood cells. 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]. Shimomura T, et al. MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol Cancer Ther. 2010 Jan;9(1):157-66.

溶解度数据	In Vitro: DMSO : 12.5 mg/mL (27.06 mM; Need ultrasonic)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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