An orally available

A-674563 – 1 mg

Brand:
Cayman
CAS:
552325-73-2
Storage:
-20
UN-No:
Non-Hazardous - /

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki = 11 nM for Akt1).{26942} It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families.{26942} A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4 µM.{26942} In vivo, 40 mg/kg/day A-674563 in combination with 15 mg/kg/day paclitaxel (Item No. 10461) was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.{26942}  

 

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Description

An orally available, reversible inhibitor of Akt (Ki = 11 nM for Akt1); also inhibits PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively; reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells both in vitro and in vivo

Formal name: αS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-benzeneethanamine

Synonyms: 

Molecular weight: 358.4

CAS: 552325-73-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Kinase Inhibitors|PKA||Product Type|Biochemicals|Kinase Inhibitors|PKB/Akt||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cell Signaling|cAMP Signaling||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling

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