| Identification | Back Directory | [Name]
GSK-2110183C | [CAS]
1047644-62-1 | [Synonyms]
Delitinib
Afuresertib
GSK2110183C
GSK-2110183C
GSK 2110183C
GSK-2110183C USP/EP/BP
GSK-2110183 Afuresertib
Afuresertib(GSK2110183C)
Afuresertib, GSK-2110183, GSK-2110183B
N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide
2-Thiophenecarboxamide, N-[(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)- | [EINECS(EC#)]
1592732-453-0 | [Molecular Formula]
C18H17Cl2FN4OS | [MDL Number]
MFCD26961098 | [MOL File]
1047644-62-1.mol | [Molecular Weight]
427.32 |
| Chemical Properties | Back Directory | [Boiling point ]
535.1±50.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
DMSO:62.5(Max Conc. mg/mL);146.26(Max Conc. mM)
Ethanol:85.0(Max Conc. mg/mL);198.91(Max Conc. mM) | [form ]
Powder | [pka]
13.03±0.46(Predicted) | [color ]
White to off-white | [InChI]
InChI=1S/C18H17Cl2FN4OS/c1-25-16(14(19)9-23-25)13-7-15(27-17(13)20)18(26)24-12(8-22)6-10-3-2-4-11(21)5-10/h2-5,7,9,12H,6,8,22H2,1H3,(H,24,26)/t12-/m0/s1 | [InChIKey]
AFJRDFWMXUECEW-LBPRGKRZSA-N | [SMILES]
C1(C(N[C@@H](CC2=CC=CC(F)=C2)CN)=O)SC(Cl)=C(C2N(C)N=CC=2Cl)C=1 |
| Hazard Information | Back Directory | [Uses]
Afuresertib is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma. | [Definition]
ChEBI: N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methyl-3-pyrazolyl)-2-thiophenecarboxamide is a member of amphetamines. | [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 result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover 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 treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts[1]. | [IC 50]
Akt2: 2 nM (Ki); Akt3: 2.6 nM (Ki); Akt1 E17K mutant: 0.2 nM (IC50); PKCη: 210 nM (IC50); PKC-βI: 430 nM (IC50); PKCθ: 510 nM (IC50); ROCK: 100 nM (IC50) | [storage]
Store at -20°C, protect from light, stored under nitrogen |
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