产品
编 号：F370510
分子式：C23H31N5O4
分子量：441.52
分子式：C23H31N5O4
分子量：441.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 501010-06-6
产品详情
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.
体内研究：
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.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 Ki of 4.4±1.6 nM.GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3.
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.
体内研究：
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.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 Ki of 4.4±1.6 nM.GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3.
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