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Afuresertib

Cat. No. M5308

All AbMole products are for research use only, cannot be used for human consumption.

Afuresertib Structure
Synonym:

GSK2110183; LAE002

Size Price Availability Quantity
2mg USD 63  USD63 In stock
5mg USD 85  USD85 In stock
10mg USD 125  USD125 In stock
25mg USD 210  USD210 In stock
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Quality Control & Documentation
Biological Activity

In vitro: Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib.

In vivo: Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively.

Chemical Information
Molecular Weight 427.32
Formula C18H17Cl2FN4OS
CAS Number 1047644-62-1
Solubility (25°C) DMSO 90 mg/mL
Storage -20°C, protect from light, sealed
References

[1] Tolcher AW, et al. Cancer Chemother Pharmacol. Phase I study of the MEK inhibitor trametinib in combination with the AKT inhibitor afuresertib in patients with solid tumors and multiple myeloma.

[2] Spencer A, et al. Blood. The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma.

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  Catalog
Abmole Inhibitor Catalog




Keywords: Afuresertib, GSK2110183; LAE002 supplier, Akt, inhibitors, activators

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