Afuresertib HCl (GSK-2110183)

    • Catalog No.:MC0751
      • CasNo:
      • 1047645-82-8
      • MolecularFormula:
      • C18H18Cl3FN4OS
      • Purity:
      • >98%
      • Target:
      • PKA
      • IC50:
      • Ki: 0.08 nM (AKT1), 2 nM (AKT2), 2.6 nM (AKT3)[1] IC50: 0.2 nM (AKT1E17K), 1.3 nM (PKA), 0.9 nM (PKG1α), 4 nM (PKG1β)[1]
      • In Vitro:
      • Afuresertib (GSK2110183) shows concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both BT474 and LNCaP cell lines. GSK2110183 consistently has potent anti-proliferative effects on a variety of hematological malignancies. Overall 65% of the hematological cell lines are sensitive to GSK2110183 (EC50<1 µM). Among solid tumor cell lines, 21% have EC50<1 µM in response to GSK2110183[1].
      • In Vivo:
      • Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which results in 8, 37 and 61% tumor growth inhibition (TGI), respectively. Mice tolerates GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recovers over the course of the study. Other tumor xenograft models which possess an activation of the AKT pathway are explored to further demonstrate compound efficacy. Mice bearing SKOV3 ovarian tumor xenografts with 10, 20 and 30 mg/kg GSK2141795 QD displays a 73, 85 or 93% TGI, respectively, compared to vehicle control. Similarly, mice treated with GSK2110183 at 10, 30 and 100 mg/kg results in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts[1].
      • Fields:
      • Afuresertib (GSK2110183) is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM). Ki: 0.08 nM (AKT1), 2 nM (AKT2), 2.6 nM (AKT3)[1] IC50: 0.2 nM (AKT1E17K), 1.3 nM (PKA), 0.9 nM (PKG1α), 4 nM (PKG1β)[1]
      • Specificity:
      • Target: PKA . Fields: Afuresertib (GSK2110183) is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM). Ki: 0.08 nM (AKT1), 2 nM (AKT2),
      • Source:
      • Rabbit
      • Dilution:
      • Ki: 0.08 nM (AKT1), 2 nM (AKT2), 2.6 nM (AKT3)[1] IC50: 0.2 nM (AKT1E17K), 1.3 nM (PKA), 0.9 nM (PKG1α), 4 nM (PKG1β)[1]
      • Concentration:
      • >98%
      • Storage Stability:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • Other Name:
      • Afuresertib,GSK 2110183,GSK2110183
      • MolecularWeight(Da):
      • 463.78
      • References:
      • [1]. 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.
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