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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Aurora Kinase-MK-5108
MK-5108

Chemical Structure : MK-5108

CAS No.: 1010085-13-8

MK-5108 (MK 5108;VX-689;VX 689;MK5108;VX689)

货号: PC-43431Not For Human Use, Lab Use Only.

MK-5108 (VX-689) is a potent, highly selective Aurora-A kinase inhibitor with IC50 of 0.064 nM.

规格 价格 库存 数量
5 mg ¥880 In stock
10 mg ¥1280 In stock
25 mg ¥1980 In stock
50 mg ¥3280 In stock
100 mg ¥5480 In stock
250 mg Get quote
1 g Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MK-5108 (VX-689) is a potent, highly selective Aurora-A kinase inhibitor with IC50 of 0.064 nM, displays robust selectivity against Aurora-B (220-fold) and Aurora-C (190-fold) in the biochemical assays.
MK-5108 (VX-689) also exhibits high selectivity for Aurora-A over a panel of 233 kinases, only one kinase (TrkA) with <100-fold selectivity.
MK-5108 (VX-689) inhibits the growth of multiple human cancer cell lines in vitro and in human cancer xenograft models.
MK-5108 (VX-689) MK-5108 significantly enhanced the efficacy of docetaxel without increasing its toxicity.

物理化学性质&存储条件

分子量 461.94
分子式 C22H21ClFN3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 6.4 mg/mL (Need warming)

Chemical Name/SMILES

Cyclohexanecarboxylic acid, 4-(3-chloro-2-fluorophenoxy)-1-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-, trans-

参考文献

1. Shimomura T, et al. Mol Cancer Ther. 2010 Jan;9(1):157-66.

2. Kretzner L, et al. Cancer Res. 2011 Jun 1;71(11):3912-20.

3. Shan W, et al. Clin Cancer Res. 2012 Jun 15;18(12):3352-65.

4. Chefetz I, et al. Cell Cycle. 2011 Jul 1;10(13):2206-14.

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