GSK-2110183C
GSK-2110183C Basic information
- Product Name:
- GSK-2110183C
- Synonyms:
-
- Afuresertib(GSK2110183C)
- Afuresertib
- GSK 2110183C
- GSK2110183C
- GSK-2110183C
- N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide
- Afuresertib, GSK-2110183, GSK-2110183B
- Delitinib
- CAS:
- 1047644-62-1
- MF:
- C18H17Cl2FN4OS
- MW:
- 427.32
- EINECS:
- 1592732-453-0
- Product Categories:
-
- Inhibitors
- Mol File:
- 1047644-62-1.mol
GSK-2110183C Chemical Properties
- 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) - pka
- 13.03±0.46(Predicted)
- form
- Powder
- 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
GSK-2110183C Usage And Synthesis
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)
GSK-2110183CSupplier
- Tel
- 18136139868; 18136139868
- jinlun@goodchemtech.cn
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- sales@boylechem.com
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