产品
编 号：F243982
分子式：C25H23N5O2S2
分子量：489.61
分子式：C25H23N5O2S2
分子量：489.61
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 195987-41-8
产品详情
生物活性：
BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.
体内研究：
Tumors from BMS-214662-treated mice have increased numbers of apoptotic cells as compared with the nontreated control mice. The AIs in HCT-116 tumors are increased 4-10-fold in BMS-214662-treated mice as compared with nontreated controls. BMS-214662 is significantly cytotoxic to both HCT-116 and EJ-1 tumor cells; the doses of BMS-214662 required to kill 90% of clonogenic tumor cells are approximately 75 and 100 mg/kg for HCT-116 and EJ-1 tumors.
体外研究：
BMS-214662 is over 1000-fold selective for farnesyl transferase, having IC50 values for inhibition of geranylgeranylation of Ras-CVLL and K-Ras of 1.3 and 2.3 μM, respectively. BMS-214662 shows good potency in inhibiting H-ras-transformed rodent cells, A2780 human ovarian carcinoma tumor cells, and HCT-116 human colon carcinoma tumor cells. BMS-214662 is the most potent apoptotic FTI known and demonstrates broad spectrum yet robust cell-selective cytotoxic activity against a panel of cell lines with diverse histology.
BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.
体内研究：
Tumors from BMS-214662-treated mice have increased numbers of apoptotic cells as compared with the nontreated control mice. The AIs in HCT-116 tumors are increased 4-10-fold in BMS-214662-treated mice as compared with nontreated controls. BMS-214662 is significantly cytotoxic to both HCT-116 and EJ-1 tumor cells; the doses of BMS-214662 required to kill 90% of clonogenic tumor cells are approximately 75 and 100 mg/kg for HCT-116 and EJ-1 tumors.
体外研究：
BMS-214662 is over 1000-fold selective for farnesyl transferase, having IC50 values for inhibition of geranylgeranylation of Ras-CVLL and K-Ras of 1.3 and 2.3 μM, respectively. BMS-214662 shows good potency in inhibiting H-ras-transformed rodent cells, A2780 human ovarian carcinoma tumor cells, and HCT-116 human colon carcinoma tumor cells. BMS-214662 is the most potent apoptotic FTI known and demonstrates broad spectrum yet robust cell-selective cytotoxic activity against a panel of cell lines with diverse histology.
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