| Identification | Back Directory | [Name]
GSK2110183B | [CAS]
1047645-82-8 | [Synonyms]
GSK2110183B
GSK-2110183B
GSK 2110183B
Afuresertib HCl
GSK2110183 hydrochloride
GSK-2110183 hydrochloride
GSK 2110183 hydrochloride
Afuresertib (hydrochloride)
Afuresertib HCl (GSK2110183)
Afuresertib hydrochloride GSK2110183
GSK 2110183 hydrochloride - Afuresertib hydrochloride
Afuresertib HCl salt, GSK-2110183 HCl salt, GSK-2110183B HCl salt
AFURESERTIB;GSK 2110183;GSK2110183;GSK 2110183 HYDROCHLORIDE; GSK2110183 HYDROCHLORIDE; GSK-2110183 HYDROCHLORIDE
(S)-N-(1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide hydrochloride
N-((S)-1-Amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide hydrochloride
N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride
2-Thiophenecarboxamide, n-[(1s)-2-amino-1-[(3-fluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-, hydrochloride (1:1) | [Molecular Formula]
C18H18Cl3FN4OS | [MOL File]
1047645-82-8.mol | [Molecular Weight]
463.78 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
DMSO:65.0(Max Conc. mg/mL);140.15(Max Conc. mM)
DMF:50.0(Max Conc. mg/mL);107.81(Max Conc. mM)
Ethanol:50.0(Max Conc. mg/mL);107.81(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.08(Max Conc. mM) | [form ]
A crystalline solid | [color ]
Yellow to brown |
| Hazard Information | Back Directory | [Uses]
Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively. It preferentially inhibits the proliferation of human cancer cell lines with Akt pathway activation and various cell lines derived from hematologic malignancies with minimal effect on glucose homeostasis. Afuresertib demonstrates activity against multiple myeloma in both preclinical and clinical models.[Cayman Chemical] | [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[2]. | [IC 50]
Akt1: 0.08 nM (Ki); 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); ROCK: 100 nM (IC50); PKCθ: 510 nM (IC50) | [storage]
Store at -20°C, protect from light, stored under nitrogen |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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