BMS-214662 hydrochloride 

BMS-214662 hydrochloride is an inhibitor of farnesyltransferase (Farnesyl Transferase). BMS-214662 hydrochloride can effectively block the localization and function of Ras proteins on the cell membrane by inhibiting the prenylation modification of Ras proteins, thereby exerting anti-tumor activity. The IC₅₀ value of BMS-214662 hydrochloride for H-Ras is 1.3 nM, and for K-Ras it is 8.4 nM. BMS-214662 hydrochloride can be used in the research of tumor diseases related to Ras^[1][2].

IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)^[1]

BMS-214662 对法尼基转移酶的选择性超过 1000 倍，抑制 Ras-CVLL 和 K-Ras 的香叶基香叶基化的 IC₅₀ 值分别为 1.3 和 2.3 μM^[1]。BMS-214662 在抑制 H-ras 转化的啮齿动物细胞、A2780 人卵巢癌肿瘤细胞和 HCT-116 人结肠癌肿瘤细胞方面表现出良好的效力。BMS-214662 是已知最有效的凋亡 FTI，对一组具有不同组织学的细胞系表现出广谱但强大的细胞选择性细胞毒活性^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

与未处理的对照小鼠相比，经 BMS-214662 处理的小鼠肿瘤中的凋亡细胞数量增加。与未处理的对照组相比，BMS-214662 处理的小鼠中 HCT-116 肿瘤的 AI 增加了 4-10 倍。BMS-214662 对 HCT-116 和 EJ-1 肿瘤细胞均具有显著的细胞毒性；对于 HCT-116 和 EJ-1 肿瘤，杀死 90% 克隆形成肿瘤细胞所需的 BMS-214662 剂量约为 75 和 100 mg/kg^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

526.07

C₂₅H₂₄ClN₅O₂S₂

195981-08-9

固体

Off-white to light brown

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Hunt JT, et al. Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity. J Med Chem. 2000 Oct 5;43(20):3587-95.  [Content Brief]

  [2]. Rose WC, et al. Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res. 2001 Oct 15;61(20):7507-17.  [Content Brief]