mTOR-IN-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

mTOR inhibitor-3 是一种有效的 mTOR 抑制剂，Ki 值为 1.5 nM。mTOR inhibitor-3 在细胞实验及体内药代动力学 (PK)/药效学 (PD) 实验中都抑制 mTORC1 和 mTORC2。

A potent and selective mTOR inhibitor with Ki of 1.5 nM; >500-fold selectivity over closely related PI3 kinases; exhibits suitable mouse PK and demenstrates active in an NCI-PC3prostate cancer model; orally bioavailable.

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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) . 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.

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PI3K/Akt/mTOR signaling

mTOR

mTOR

Cancer

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1207358-59-5

474.5581

C25H30N8O2

>98% (HPLC)

10 mM in DMSO

CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4=NC=CC=N4)C(=N2)N5CCOCC5C

Urea, N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(2-pyrimidinyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years