PI3K/mTOR Inhibitor-9

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CAS NO:

1392421-71-4

PI3K/mTOR Inhibitor-9 (Compound 1) 是一种有效的mTOR和PI3K抑制剂，对 mTOR、PI3Kα、PI3Kγ 和 PI3Kδ 的IC₅₀分别为 38 nM、6.6 μM、6.6 μM 和 0.8 μM。

生物活性

PI3K/mTOR Inhibitor-9 (Compound 1) is a potentmTORandPI3Kinhibitor withIC₅₀values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM againstmTOR(phospho-S6 cellular assay),PI3Kα,PI3KγandPI3Kδ, respectively^[1].

IC₅₀& Target

mTOR

38 nM (IC₅₀, phospho-S6 cellular assay)

PI3Kα

6.6 μM (IC₅₀)

PI3Kβ

>10 μM (IC₅₀)

PI3Kγ

6.6 μM (IC₅₀)

PI3Kδ

0.8 μM (IC₅₀)

mTOR

16 nM (IC₅₀, Ser240/244 cellular assay)

体外研究
(In Vitro)

PI3K/mTOR Inhibitor-9 (Compound 1) shows good selectivity over the related kinases PI3Kα, β and γ, although with lower selectivity over PI3Kδ^[1].
PI3K/mTOR Inhibitor-9 inhibits CYP2D6 (IC₅₀= 1.98 μM) and shows time-dependent inhibition (TDI) of CYP3A4 (rate of enzyme inhibition, k_obs= 0.080 /min)^[1].
PI3K/mTOR Inhibitor-9 shows good permeability with no sign of P-gp efflux (B-A/A-B: 0.95)^[1].

分子量

433.51

Formula

C₂₃H₂₇N₇O₂

CAS 号

1392421-71-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.