CZ415 是一种有效的高选择性 mTOR 抑制剂，pIC₅₀ 为 8.07。CZ415 抑制 mTORC1 和 mTORC2 复合体。

CZ415 is a potent and highly selective mTOR inhibitor with a pIC 50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.

Solid

mTOR 8.07 (pIC50) mTORC1

Inhibition of phosphorylation for both downstream targets results in 14.5 nM IC50 for pS6RP and 14.8 nM for pAKT. The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 hours in stimulated human whole blood and the resulting IC50 is 226 nM. As a predictor for cardiotoxicity, the activity of CZ415 against the human cardiac ion channel hERG is assessed in a whole-cell patch-clamp assay in HEK293 cells resulting in an IC50 of 48 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

CZ415 is a highly selective mTOR inhibitor showing in vivo efficacy in a collagen induced arthritis (CIA) model. For full characterization of CZ415 and to enable improved dose predictions, the pharmacokinetic (PK) profile is assessed in rat. PK and oral bioavailability are determined after of 1 mg/kg intravenous (iv) bolus and 3 mg/kg oral (po) administration. The observed plasma clearance, corresponding to 45% liver blood flow, suggests that sufficient levels of free compound are circulating in the animal over time. The oral uptake is rapid with a T max max of 0.5 h and bioavailability F = 44% indicates very good absorption from the gut. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Cansfield AD, et al. CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model. ACS Med Chem Lett. 2016 Jun 10;7(8):768-73.

In Vitro: DMSO : 100 mg/mL (217.60 mM; Need ultrasonic)配制储备液