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FTI-2148 diTFA

CAS No. : 817586-01-9

MCE 站：FTI-2148 diTFA

产品活性：FTI-2148 diTFA 是 RAS C 末端修饰的法呢基转移酶 (FT-1) 和香叶基转移酶 1 (GGT-1) 的抑制剂，抑制 FT-1 和 GGT-1 的 IC₅₀ 分别为 1.4 nM 和 1.7 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Farnesyl Transferase

In Vitro: FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells.
FTI-2148 diTFA is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC₅₀ values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I.

In Vivo: FTI-2148 (intraperitoneal?injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model.
FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model.
FTI-2148 (subcutaneous?injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a?ras?transgenic mouse model.
FTI-2148 (subcutaneous?injection; 100 mg/kg/day; 4 days) results in 85–88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo?settings.

相关产品：Tipifarnib  |  Lonafarnib  |  FTI-277 hydrochloride  |  L-778123 hydrochloride  |  Lapaquistat acetate  |  FTI-2153  |  Arglabin  |  BMS-214662  |  ABT-100  |  FTI 276  |  FTI-2148  |  Manumycin A  |  Tectol  |  LNK754  |  Prenyl-IN-1  |  RPR107393 free base  |  YM-53601 free base

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