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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Farnesyl transferase (FTase)-BMS-214662
BMS-214662

Chemical Structure : BMS-214662

CAS No.: 195987-41-8

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BMS-214662 (BMS214662)

货号: PC-24422Not For Human Use, Lab Use Only.

BMS-214662 is a potent, selective farnesyltransferase (FTase) inhibitor with IC50 of 1.35 nM, inhibits anchorage-independent growth of H-ras transformed NIH3T3 cells in soft agar EC50 of 25 nM.

规格 价格 库存 数量
5 mg ￥2480 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg 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

BMS-214662 is a potent, selective farnesyltransferase (FTase) inhibitor with IC50 of 1.35 nM, inhibits anchorage-independent growth of H-ras transformed NIH3T3 cells in soft agar EC50 of 25 nM.
BMS-214662 is over 1000-fold selective over the related enzyme GGT1.
BMS-214662 has IC50 values for inhibition of geranylgeranylation of Ras-CVLL and K-Ras of 1.3 and 2.3 μM, respectively.
BMS-214662 reversed the H-Ras-transformed phenotype but not that of K-Ras or other oncogenes.
BMS-214662 (300 mg/kg) achieved curative efficacy when given orally in the HCT-116 human colon tumor model.
BMS-214662 demonstrated broad spectrum activity against human tumors, but murine tumors were not as sensitive.

物理化学性质&存储条件

分子量 489.61
分子式 C25H23N5O2S2
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

10 mM in DMSO
Chemical Name/SMILES

(R)-1-((1H-Imidazol-5-yl)methyl)-3-benzyl-4-(thiophen-2-ylsulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile

参考文献

1. Rose WC, et al. Cancer Res. 2001 Oct 15;61(20):7507-17.

2. Hunt JT, et al. J Med Chem. 2000 Oct 5;43(20):3587-95.

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