AKTI-2008

Name	AKTI-2008
Synonyms	Akti_2008 AKTI-2008 Akt1Akt2-IN-17 Akt1 and Akt2-IN-1 3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one 3-phenyl-2-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-1,6-naphthyridin-5(6H)-one 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]-
CAS	893422-47-4

Molecular Formula	C33H29N7O
Molar Mass	539.63
Storage Condition	2-8℃
In vitro study	Consistent with the allosteric mode of inhibition, Akt1 and Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC 50 =1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1 and Akt2-IN-1 (Compound 17) has moderate activity in an hERG binding assay (IC 50 =5610 nM) and is a substrate for human P-glycoprotein.
In vivo study	Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1 and Akt2-IN-1 (Compound 17) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1 and Akt2-IN-1 (Compound 17) has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1 and Akt2-IN-1 (Compound 17) 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 and Akt2-IN-1 (Compound 17), 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 and Akt2-IN-1 (Compound 17) is well tolerated in mice and shows high levels of Akt inhibition in mouse lung.

Last Update：2024-01-02 23:10:35

biological activity

Akt1 and Akt2-IN-1 are potent allosteric inhibitors of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM).

Last Update：2024-04-09 20:52:54

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Product Name: AKTI-2008 Visit Supplier Webpage Request for quotation
CAS: 893422-47-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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AKTI-2008

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