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GGTI-2418

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Chemical Structure| 501010-06-6 同义名 : -
CAS号 : 501010-06-6
货号 : A765852
分子式 : C23H31N5O4
纯度 : 99%+
分子量 : 441.523
MDL号 : MFCD25976818
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(271.79 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The ability of the GTPases to mediate these tumorigenic events requires their posttranslational modification with farnesyl and geranylgeranyl lipids. The enzymes responsible for these modifications is geranylgeranyltransferase I (GGTI), and inhibitors of GGTI have been developed as potential anticancer drugs. GGTI-2418 is a potent and selective peptidomimetic inhibitor of GGTI. In vitro, GGTI-2418 inhibits GGTI with IC50 of 9.5 ± 2.0 nM. And it demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki value of 4.4 ± 1.6 nM. Tumors from mice treated with 100 mg/kg GGTI-2418 intraperitoneally daily or 200 mg/kg every third day grew to only average tumor sizes of 139 ± 17 or 276 ± 26 mm3, respectively, corresponding to tumor growth inhibitions of 94% and 77%, respectively (P < 0.005 for both). These data clearly indicate that GGTI-2418 potently inhibits the growth of breast tumor xenografts with either daily or intermittent dosing. Moreover, in seven mice with a total of 17 tumors, treatment with 100 mg/kg GGTI-2418 resulted in tumor regression between 34 and 100%, with an average of 60% ± 4%[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.32mL

2.26mL

1.13mL

22.65mL

4.53mL

2.26mL
参考文献

[1]Kazi A, Carie A, Blaskovich MA, et al. Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy. Mol Cell Biol. 2009;29(8):2254‐2263