FGTI-2734 mesylate
目录号: PL13907 纯度: ≥99%
CAS No. :2702297-24-1
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中文名称
FGTI-2734 mesylate
英文名称
FGTI-2734 mesylate
英文别名
FGTI-2734 mesylate
Cas No.
2702297-24-1
分子式
C27H35FN6O5S2
分子量
606.73
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
FGTI-2734 mesylate 是 RAS C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT) 抑制剂,对 FT 和 GGT 的 IC50s 分别为 250 nM 和 520 nM。FGTI-2734 mesylate 可以阻断 KRAS 的膜定位,从而解决 KRAS 耐药性问题,并抑制突变的 KRAS 胰腺肿瘤。
生物活性
FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC 50 s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
性状
Solid
IC50 & Target[1][2]
IC50: 250 nM (FT) and 520 nM (GGT)
体外研究(In Vitro)
FGTI-2734 mesylate (1-30 μM; 72 hours) induces apoptosis in mutant KRAS-dependent, but not mutant KRAS- independent, human cancer cells.
FGTI-2734 mesylate (3-30 μM; 72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
FGTI-2734 mesylate (intraperitoneally; 100 mg/kg/day for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Kazi A, et al. Dual farnesyl and geranylgeranyl transferase inhibitor thwarts mutant KRAS-driven patient-derived pancreatic tumors. Clin Cancer Res. 2019 Jun 21.
溶解度数据
In Vitro: DMSO : 75 mg/mL (123.61 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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