CAS NO: | 937174-76-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | GSK-690693 is an ATP-competitivepan-Aktinhibitor withIC50s of 2 nM, 13 nM, 9 nM forAkt1,Akt2andAkt3, respectively. GSK-690693 is also anAMPKinhibitor, affects Unc-51-likeautophagyactivating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation[1][2][3]. | |||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other families. However, GSK690693 is less selective for members of the AGC kinase family including PKA, PrkX, and PKC isozymes with IC50of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50of 50 nM and 81 nM, respectively, and PAK4, 5, and 6 from the STE family with IC50of 10 nM, 52 nM, and 6 nM, respectively. GSK690693 inhibits the phosphorylation of GSK3β in tumor cells with IC50ranging from 43 nM to 150 nM. GSK690693 treatment leads to a dose-dependent increase in the nuclear accumulation of the transcription factor FOXO3A. GSK690693 potently inhibits the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively. GSK690693 treatment induces apoptosis at concentrations >100 nM in both LNCaP and BT474 cells[1]. Consistent with the role of AKT in cell survival, GSK690693 induces apoptosis in sensitive ALL cell lines[2]. | |||||||||||||||||
体内研究 (In Vivo) | A single administration of GSK690693 inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts in a dose- and time-dependent manner. Similarly, GSK690693 induces a reduction in phosphorylation of the Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 also results in an acute increase in blood glucose, returning to baseline 8 to 10 hours after drug administration. Administration of GSK690693 induces reductions in phosphorylated Akt substrates in vivo, and potently inhibits the growth of human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts, with maximal inhibition of 58% to 75% at the dose of 30 mg/kg/day[1]. GSK690693 exhibits efficacy irrespective of the mechanism of Akt activation involved. GSK690693 is most effective in delaying tumor progression in Lck-MyrAkt2 mice expressing a membrane-bound, constitutively active form of Akt[3]. | |||||||||||||||||
Clinical Trial | ||||||||||||||||||
分子量 | 425.48 | |||||||||||||||||
性状 | Solid | |||||||||||||||||
Formula | C21H27N7O3 | |||||||||||||||||
CAS 号 | 937174-76-0 | |||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | |||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 20 mg/mL(47.01 mM;ultrasonic and warming and heat to 60℃) H2O : 5 mg/mL(11.75 mM;ultrasonic and adjust pH to 5 with HCl) 配制储备液
* 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。 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
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