GGTI-2418|cas:501010-06-6|西域试剂

GGTI-2418,98.04%

产品编号：Bellancom-16231| CAS NO：501010-06-6| 分子式：C₂₃H₃₁N₅O₄| 分子量：441.52

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16231	￥1400.00	杭州北京（现货）
Bellancom-16231	￥2300.00	杭州北京（现货）
Bellancom-16231	￥4500.00	杭州北京（现货）
Bellancom-16231	￥7700.00	杭州北京（现货）
Bellancom-16231	￥13500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

GGTI-2418

产品介绍

GGTI-2418 是一种高效，竞争性和选择性的香叶基香叶基转移酶 I (GGTase I) 抑制剂。GGTI-2418 抑制 GGTase I 和 FTase 活性，IC₅₀ 分别为 9.5 nM 和 53 μM。GGTI-2418 还增强 p27(Kip1) 并诱导乳腺肿瘤显着消退。

生物活性

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC₅₀s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors.

体外研究

GGTI-2418 inhibits GGTase I and FTase activities with IC₅₀s of 9.5±2.0 nM and 53±11 μM, respectively, a 5,600-fold selectivity toward inhibition of GGTase I versus FTase. GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a K_i of 4.4±1.6 nM.
GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3.

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

Western Blot Analysis

Cell Line:	HeLa cells
Concentration:	10-15 μM
Incubation Time:	16 hours
Result:	Delocalized FBXL2 and stabilized IP3R3.

体内研究
(In Vivo)

GGTI-2418 (100 mg/kg daily or 200 mg/kg every third day; 15 days) significantly inhibits the growth of breast tumor xenografts in nude mice with MDA-MB-231 xenografts.
GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice.
GGTI-2418 inhibits the geranylgeranylation of Rap1 and causes a dramatic decrease in S473 phosphorylation of Akt. GGTI-2418 also upregulates p27 levels in vivo.

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

Animal Model:	Nude mice implanted with MDA-MB-231 breast cancer tumors
Dosage:	100 mg/kg daily or 200 mg/kg every third day
Administration:	Injected intraperitoneally; 15 days
Result:	Inhibited the growth of breast tumor xenografts.

Animal Model:	ErbB2 transgenic mice
Dosage:	100 mg/kg/day
Administration:	Subcutaneously; 5 days
Result:	Halted tumor growth and induced massive tumor regression. Tumor decreased by 76% following GGTI-2418 treatment.

体内研究

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

Animal Model:	Nude mice implanted with MDA-MB-231 breast cancer tumors
Dosage:	100 mg/kg daily or 200 mg/kg every third day
Administration:	Injected intraperitoneally; 15 days
Result:	Inhibited the growth of breast tumor xenografts.

Animal Model:	ErbB2 transgenic mice
Dosage:	100 mg/kg/day
Administration:	Subcutaneously; 5 days
Result:	Halted tumor growth and induced massive tumor regression. Tumor decreased by 76% following GGTI-2418 treatment.

体内研究

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

Animal Model:	Nude mice implanted with MDA-MB-231 breast cancer tumors
Dosage:	100 mg/kg daily or 200 mg/kg every third day
Administration:	Injected intraperitoneally; 15 days
Result:	Inhibited the growth of breast tumor xenografts.

Animal Model:	ErbB2 transgenic mice
Dosage:	100 mg/kg/day
Administration:	Subcutaneously; 5 days
Result:	Halted tumor growth and induced massive tumor regression. Tumor decreased by 76% following GGTI-2418 treatment.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (283.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2649 mL	11.3245 mL	22.6490 mL
5 mM	0.4530 mL	2.2649 mL	4.5298 mL
10 mM	0.2265 mL	1.1325 mL	2.2649 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。-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: ≥ 2.08 mg/mL (4.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.71 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.71 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.71 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。