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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Farnesyl transferase (FTase)-FGTI-2734
FGTI-2734

Chemical Structure : FGTI-2734

CAS No.: 1247018-19-4

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FGTI-2734 (FGTI2734)

货号: PC-73014Not For Human Use, Lab Use Only.

FGTI-2734 (FGTI2734) is a potent, CAAX tetrapeptide RAS C-terminal mimetic as dual farnesyltransferase (FT) and geranylgeranyltransferase-1 (GGT-1) inhibitor with IC50 of 250 and 520 nM, respectively.

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5 mg ￥1380 In stock
10 mg ￥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

FGTI-2734 (FGTI2734) is a potent, CAAX tetrapeptide RAS C-terminal mimetic as dual farnesyltransferase (FT) and geranylgeranyltransferase-1 (GGT-1) inhibitor with IC50 of 250 and 520 nM, respectively.
FGTI-2734 inhibits both protein prenylation and membrane localization of KRAS and NRAS in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells, but not the highly selective FTI-2148 or GGTI-2418.
FGTI-2734 inhibits the prenylation of both HDJ2 and RAP1A.
FGTI-2734 inhibits RAF-1 kinase activity although cytosolic KRAS binds RAF-1, it requires KSR and the membrane environment to fully activate RAF-1.
FGTI-2734 induces apoptosis in mutant KRAS-dependent, but not mutant KRAS-independent human cancer cells.
FGTI-2734 inhibits the in vivo growth of mutant KRAS-dependent but not mutant KRAS–independent human tumors in mouse xenograft models (100 mg/kg, i.p.), also inhibits the growth of mutant KRAS PDXs from patients with pancreatic cancer.

物理化学性质&存储条件

分子量 510.632
分子式 C26H31FN6O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(2-((4-cyano-2-fluorophenyl)((1-methyl-1H-imidazol-5-yl)methyl)amino)ethyl)-N-(cyclohexylmethyl)pyridine-2-sulfonamide

参考文献

1. Sebti SM, et al. Clin Cancer Res. 2019 Jun 21. pii: clincanres.3399.2018. doi: 10.1158/1078-0432.CCR-18-3399.

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