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A-443654

Cat. No. M14830
A-443654 Structure
Size Price Availability
5mg USD 330  USD330 4-7 Days
10mg USD 590  USD590 4-7 Days
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Quality Control & Documentation
Biological Activity

A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).

Chemical Information
Molecular Weight 397.47
CAS Number 552325-16-3
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Mandi Gandelman, et al. The AKT modulator A-443654 reduces α-synuclein expression and normalizes ER stress and autophagy

[2] Gi Uk Jeong, et al. Aurora kinase A promotes hepatitis B virus replication and expression

[3] Marina Glvez-Peralta, et al. Context-dependent antagonism between Akt inhibitors and topoisomerase poisons

[4] Xuesong Liu, et al. Akt inhibitor a-443654 interferes with mitotic progression by regulating aurora a kinase expression

[5] E K-H Han, et al. Akt inhibitor A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibition

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Keywords: A-443654 supplier, Akt, inhibitors, activators


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