FGTI-2734 mesylate|cas:2702297-24-1|西域试剂

FGTI-2734 mesylate,99.05%

产品编号：Bellancom-128350A| CAS NO：2702297-24-1| 分子式：C₂₇H₃₅FN₆O₅S₂| 分子量：606.73

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货号	价格	库存与货期
Bellancom-128350A	￥3500.00	杭州北京（现货）
Bellancom-128350A	￥6500.00	杭州北京（现货）
Bellancom-128350A	￥20000.00	杭州北京（现货）
Bellancom-128350A	￥35000.00	杭州北京（现货）

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FGTI-2734 mesylate

产品介绍

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 IC₅₀s 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line:	MiaPaCa2, L3.6pl, Calu6 cells
Concentration:	1, 3, 10, 30 μM
Incubation Time:	72 hours
Result:	Induced apoptosis in mutant KRAS-dependent human cancer cell lines

Western Blot Analysis

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 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.

西域 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
Dosage:	100 mg/kg
Administration:	Intraperitoneally; daily; for 18 to 25 days
Result:	Inhibited tumor growth in mutant KRAS-dependent tumors.

体内研究

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.

西域 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
Dosage:	100 mg/kg
Administration:	Intraperitoneally; daily; for 18 to 25 days
Result:	Inhibited tumor growth in mutant KRAS-dependent tumors.

体内研究

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.

西域 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
Dosage:	100 mg/kg
Administration:	Intraperitoneally; daily; for 18 to 25 days
Result:	Inhibited tumor growth in mutant KRAS-dependent tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : 75 mg/mL (123.61 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6482 mL	8.2409 mL	16.4818 mL
5 mM	0.3296 mL	1.6482 mL	3.2964 mL
10 mM	0.1648 mL	0.8241 mL	1.6482 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 (sealed storage, away from moisture)。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3 mg/mL (4.94 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (4.94 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 3 mg/mL (4.94 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (4.94 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3 mg/mL (4.94 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (4.94 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 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。