Chemical Structure : BMS-214662
CAS No.:
195987-41-8
BMS-214662
(BMS214662)
Catalog No.: 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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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489.61
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Formula
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C25H23N5O2S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
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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