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FTI-2148
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FTI-2148图片
CAS NO:251577-09-0
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
FTI-2148 是 RAS C 末端修饰的法呢基转移酶 (FT-1) 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。
生物活性

FTI-2148 is aRASC-terminal mimetic dual farnesyl transferase(FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively[1].

IC50& Target

IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)[1]

体外研究
(In Vitro)

FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells[1].
FTI-2148 is againstP. falciparumPFT, Mammalian PFT and Mammalian PGGT-I with IC50values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I[2].

Western Blot Analysis[]

Cell Line:KRAS HRAS, and NRAS-transformed NIH3T3 cells
Concentration:30 μM
Incubation Time:
Result:Inhibited the prenylation of KRAS and NRAS.
体内研究
(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[1].
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[1].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model[1].
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[3].

Animal Model:Ras transgenic mouse model[3]
Dosage:100 mg/kg/day
Administration:Subcutaneous injection; 100 mg/kg/day; 14 days
Result:Induced regression by 87 ± 3% of mammary carcinomas in mice.
分子量

452.57

Formula

C24H28N4O3S

CAS 号

251577-09-0

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.