Afuresertib (hydrochloride)

Afuresertib hydrochloride (GSK 2110183 hydrochloride) 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[1][2].

Product Specifications

CAS Number

[1047645-82-8]

Product Name Alternative

GSK2110183 (hydrochloride) ; LAE002 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Akt; PKC; ROCK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton; Epigenetics; PI3K/Akt/mTOR; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Afuresertib-hydrochloride.html

Purity

99.95

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN.[H]Cl

Molecular Formula

C18H18Cl3FN4OS

Molecular Weight

463.78

Precautions

H302, H315, H319, H335

References & Citations

[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