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Uprosertib (GSK2141795)

Cat. No. M6044
Uprosertib (GSK2141795) Structure
Synonym:

GSK795; Uprosertib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 100  USD100 In stock
5mg USD 90  USD90 In stock
10mg USD 160  USD160 In stock
25mg USD 300  USD300 In stock
50mg USD 565  USD565 In stock
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Quality Control & Documentation
Biological Activity

Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3 respectively.

Chemical Information
Molecular Weight 429.25
Formula C18H16Cl2F2N4O2
CAS Number 1047634-65-0
Solubility (25°C) DMSO 30 mg/mL
Storage -20°C, sealed
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] Cheraghchi-Bashi A, et al. Oncotarget. A putative biomarker signature for clinically effective AKT inhibition: correlation of in vitro, in vivo and clinical data identifies the importance of modulation of the mTORC1 pathway.

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Keywords: Uprosertib (GSK2141795), GSK795; Uprosertib supplier, Akt, inhibitors, activators


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