CAS NO: | 1207358-59-5 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | mTORinhibitor-3 is a remarkably selectivemTORinhibitor with aKiof 1.5 nM.mTORinhibitor-3 suppressesmTORC1andmTORC2in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments. | ||||||||||||||||
IC50& Target[2] |
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体外研究 (In Vitro) | mTOR inhibitor-3 (Compound 12i) inhibits mTOR with a Kiof 1.5 nM, 500-fold selectivity over closely related PI3 kinases. mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC50s of 150 nM and 57 nM, respectively[2]. | ||||||||||||||||
体内研究 (In Vivo) | mTOR inhibitor-3 (Compound 8h) has high free plasma clearance in both mice (1818 mL/min/kg) and rats (1538 mL/min/kg in rat)[1]. mTOR inhibitor-3 (Compounds 12i) is selected for this study due to its potency, selectivity, and favorable mouse PK profile. Plasma levels of mTOR inhibitor-3 6 h following oral administration in PC3 tumor-bearing mice along with the fold decreases of phosphorylated mTORC1 and -2 substrates relative to time-matched vehicle controls. mTOR inhibitor-3 has moderate terminal elimination half-life (t1/2=1.7 h for mouse(1 mg/kg, iv)). mTOR inhibitor-3 achieves tumor stasis at the highest 200 mg/kg/day dose examined, which appears to also be approaching the limit of tolerability for this molecule[2]. | ||||||||||||||||
分子量 | 474.56 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H30N8O2 | ||||||||||||||||
CAS 号 | 1207358-59-5 | ||||||||||||||||
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 : 50 mg/mL(105.36 mM;Need ultrasonic) 配制储备液
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