Afuresertib free base · Synonyms: GSK-2110183 | GSK-2110183B

Afuresertib is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor.

For research use only. Not for human or veterinary use.

Target Akt PKC ROCK

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Afuresertib structure

CAS No.: 1047644-62-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 485.00	BP-02332-250mg	In stock	Get quote
500 mg	USD 685.00	BP-02332-500mg	In stock	Get quote
1 g	USD 885.00	BP-02332-1g	In stock	Get quote
5 g	Inquire	BP-02332-5g	In stock	Inquire
10 g	Inquire	BP-02332-10g	In stock	Inquire

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Description

Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.

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.

Identifiers

SMILES: CN1N=CC(Cl)=C1C1=C(Cl)SC(=C1)C(=O)N[C@H](CN)CC1=CC=CC(F)=C1
InChIKey: AFJRDFWMXUECEW-LBPRGKRZSA-N

Specifications

MW (average): 427.3230
Formula: C₁₈H₁₇Cl₂FN₄OS
CAS No.: 1047644-62-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659.

[2]. Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880

Same target

Search Akt

Same research area

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