2. Metabolic Enzyme/Protease
  3. Farnesyl Transferase
  4. BIM-46068

BIM-46068 是一种强效的、选择性的人脑法尼基转移酶 (FTase) 抑制剂 (IC50 = 91.4 nM)。BIM-46068 可特异性抑制 MiaPaCa-2 癌细胞中的 Ras 加工。BIM-46068 可用于胰腺癌的研究。

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BIM-46068

BIM-46068 Chemical Structure

CAS No. : 201487-53-8

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BIM-46068 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BIM-46068 is a potent, selectively human brain Farnesyltransferase (FTase) inhibitor (IC50 = 91.4 nM). BIM-46068 can specifically inhibit Ras processing in MiaPaCa-2 cancer cells. BIM-46068 can be used for the study of pancreatic cancer[1].

体外研究
(In Vitro)

BIM-46068 (0.1-10 µM，48 小时) 特异性抑制 MiaPaCa-2 癌细胞中 Ras 的加工[1]。
BIM-46068 (96 小时) 抑制携带野生型 Ras 的细胞以及携带不同突变型 Ras (K-ras、N-ras 或 H-ras) 的细胞的生长，并有效抑制多药耐药细胞系 T24R[1]。

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

BIM-46068 相关抗体:

Western Blot Analysis[1]

Cell Line: MiaPaCa-2 cells
Concentration: 0.1 µM, 1 µM, 10 µM
Incubation Time: 48 h
Result: Caused a change in the electrophoretic migration rate of H-Ras protein in MiaPaCa-2 cells, from rapid migration (farnesylated form) to slow migration (unfarnesylated form).
体内研究
(In Vivo)

BIM-46068 (1-30 mg/kg，腹腔注射，每日一次，持续 10 天) 以剂量依赖的方式显著降低肿瘤生长，并且在最高剂量 (30 mg/kg) 下未观察到体重减轻或死亡等毒性迹象[1]。

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

Animal Model: Nude mice were implanted s.c. with MiaPaCa-2 cells (5 × 106), a human pancreatic tumor cell line expressing mutated K-ras[1].
Dosage: 1 mg/kg, 10 mg/kg, 30 mg/kg
Administration: I.p., once daily for 10 days
Result: Significantly reduced tumor growth in a dose-dependent manner.
On day 34 post-implantation, the mean tumor volume in the 30 mg/kg group was reduced by 50% compared to the control group.
分子量

494.78

Formula

C21H42N4O3S3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BIM-46068 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

BIM-46068201487-53-8BIM46068BIM 46068Farnesyl TransferaseFtaseFarnesyltransferaseFTaseRas proteinH-RasK-RasN-RasInhibitorinhibitorinhibit

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产品名称：
BIM-46068
目录号：
HY-117893
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