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A-674563

Cat. No. M2132
A-674563 Structure
Size Price Availability Quantity
5mg USD 250 In stock
10mg USD 390 In stock
50mg USD 1180 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

A-674563 is a potent selective Akt1 (Protein Kinase B) inhibitor. A-674563 also shows inhibitory activity against PKA and CDK2 with IC50 values of 16nM and 46nM respectively. A-674563 has a significant effect on depolarization of purkinje fiber in an in vitro assay, and severe CV toxicity (e.g. hypotension) in vivo. A-674563 induced Akt blockade results in decreased STS cell downstream target phosphorylation and tumor cell growth inhibiton. A-674563 (0-30 µM) reduces the phosphorylation of GSK3α/β, TSC2, mTOR, and ribosomal protein S6 in a dose-dependent fashion in MiaPaCa-2 cells in vitro. Furthermore, A-674563 inhibits hERG ion channels in vitro and causes acute hypotension in vivo. A674563-treated (20 mg/kg/bid, p.o.) mice exhibits slower tumor growth and more than 50% decrease in the tumor volume at the termination of the study compared with that in control group.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 358.44
Formula C22H22N4O
CAS Number 552325-73-2
Purity >99%
Solubility DMSO 70 mg/mL
Water 70 mg/mL
Storage at -20°C
References

Synthesis and evaluation of indazole based analog sensitive Akt inhibitors.
Okuzumi T, et al. Mol Biosyst. 2010 Aug;6(8):1389-402. PMID: 20582381.

Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.
Luo Y, et al. Mol Cancer Ther. 2005 Jun;4(6):977-86. PMID: 15956255.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: A-674563 supplier, Akt, inhibitors

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