Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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. GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 765 | 5日内发货 | ||
25 mg | ¥ 4,980 | 8-10周 | ||
50 mg | ¥ 6,470 | 8-10周 | ||
100 mg | ¥ 11,300 | 8-10周 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,470 | 5日内发货 |
产品描述 | GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), showing inhibitory activities with IC50 values of 9.5 nM for GGTase I and 53 μM for FTase, respectively. Additionally, it enhances p27(Kip1) expression and induces significant regression of breast tumors. |
靶点活性 | FTase:53 μM , GGTase I:9.5 nM |
体外活性 | GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4±1.6 nM.?GGTi-2418 (10-15 μM;?16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3.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. |
体内活性 | 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.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. |
分子量 | 441.52 |
分子式 | C23H31N5O4 |
CAS No. | 501010-06-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (283.11 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2649 mL | 11.3245 mL | 22.649 mL | 56.6226 mL |
5 mM | 0.453 mL | 2.2649 mL | 4.5298 mL | 11.3245 mL | |
10 mM | 0.2265 mL | 1.1325 mL | 2.2649 mL | 5.6623 mL | |
20 mM | 0.1132 mL | 0.5662 mL | 1.1325 mL | 2.8311 mL | |
50 mM | 0.0453 mL | 0.2265 mL | 0.453 mL | 1.1325 mL | |
100 mM | 0.0226 mL | 0.1132 mL | 0.2265 mL | 0.5662 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GGTI-2418 501010-06-6 Metabolism Transferase GGTI 2418 GGTI2418 Inhibitor inhibitor inhibit