FGTI-2734

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FGTI-2734  纯度: 99.48%

FGTI-2734 是 RAS C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT-1) 抑制剂，对 FT 和 GGT-1 的 IC50s 分别为 250 nM 和 520 nM。 FGTI-2734 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。

FGTI-2734

FGTI-2734 Chemical Structure

CAS No. : 1247018-19-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3930 In-stock
5 mg ￥3500 In-stock
10 mg ￥6500 In-stock
50 mg ￥20000 In-stock
100 mg ￥35000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

FGTI-2734 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library

生物活性

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1].

IC50 & Target

IC50: 250 nM (FT) and 520 nM (GGT-1)[1]
体外研究
(In Vitro)

FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells[1].
FGTI-2734 (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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: MiaPaCa2, L3.6pl and Calu6 cells
Concentration: 1, 3, 10, 30 μM
Incubation Time: 72 hours
Result: Induced CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.

Western Blot Analysis[1]

Cell Line: KRAS, HRAS, and NRAS-transformed NIH3T3 cells
Concentration: 3, 10, 30 μM
Incubation Time: 72 hours
Result: Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.

体内研究
(In Vivo)

FGTI-2734 (intraperitoneally; 100 mg/kg/daily for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells[1]
Dosage: 100 mg/kg
Administration: Intraperitoneally; daily; for 18 to 25 days
Result: Inhibited tumor growth in mutant KRAS-dependent tumors.

分子量

510.63

Formula

C26H31FN6O2S
CAS 号

1247018-19-4
运输条件

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

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (97.92 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9584 mL 9.7918 mL 19.5837 mL
5 mM 0.3917 mL 1.9584 mL 3.9167 mL
10 mM 0.1958 mL 0.9792 mL 1.9584 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 7.5 mg/mL (14.69 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (14.69 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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