Akt1Akt2-IN-17

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

一种有效的选择性 Akt1 和 Akt2 双重抑制剂，IC50 分别为 3.5 nM 和 42 nM。

A potent, selective dual Akt1 and Akt2 inhibitor with IC50 of 3.5 nM and 42 nM, respectively; shows selectivity for Akt1/2 over Akt3 (IC50=1900 nM), and highly selective over other members of the AGC family of kinases; inhibit the growth of A2780 tumors in vivo; shows good physical properties and PK profile.Lung Cancer Preclinical.

Consistent with the allosteric mode of inhibition, Akt1/Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC50=1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1/Akt2-IN-1 has moderate activity in an hERG binding assay (IC50=5610 nM) and is a substrate for human P-glycoprotein.

Akt1/Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1/Akt2-IN-1 has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1/Akt2-IN-1 has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1/Akt2-IN-1 shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1/Akt2-IN-1, tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1/Akt2-IN-1 is well tolerated in mice and shows high levels of Akt inhibition in mouse lung.

Akt Inhibitor 17 | Akti_2008 | Akti 2008 | Akti2008 | Akti-2008 | Akt Inhibitor 17

PI3K/Akt/mTOR signaling

Akt

Akt

Cancer

Lung Cancer

893422-47-4

539.6296

C33H29N7O

>98% (HPLC)

DMSO: ≥ 35 mg/mL

O=C1C2=C(N=C(C3=CC=C(CN4CCC(C5=NNC(C6=NC=CC=C6)=N5)CC4)C=C3)C(C7=CC=CC=C7)=C2)C=CN1

1,6-Naphthyridin-5(6H)-one, 3-phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years