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Purity: ≥98%
GSK2110183 HCl, an analog of Afuresertib, is a potent, orally bioavailable and ATP-competitive Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. GSK2110183 HCl is an analog of afuresertib. The serine/threonine protein kinase Akt (protein kinase B) inhibitor GSK2110183 may have anti-cancer effects. The PI3K/Akt signaling pathway, tumor cell proliferation, and tumor cell apoptosis may all be inhibited by the Akt inhibitor GSK2110183, which binds to and inhibits the activity of Akt. The PI3K/Akt signaling pathway is frequently involved in the development of tumors, and aberrant PI3K/Akt signaling may play a role in the development of tumor resistance to a range of antineoplastic agents.
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| References |
:Cancer Chemother Pharmacol.2015 Jan;75(1):183-9;Blood.2014Oct 2;124(14):2162-3.
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| Molecular Formula |
C18H17CL3F2N4OS
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|---|---|
| Molecular Weight |
481.77
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| Elemental Analysis |
C, 44.88; H, 3.56; Cl, 22.07; F, 7.89; N, 11.63; O, 3.32; S, 6.65
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| CAS # |
2070009-64-0
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| Related CAS # |
GSK2110183 analog 1;1047634-63-8
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| Appearance |
Solid powder
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| SMILES |
O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=C(F)C(F)=C3)CN.[H]Cl
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| InChi Key |
BCVQLTLODHPIJM-PPHPATTJSA-N
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| InChi Code |
InChI=1S/C18H16Cl2F2N4OS.ClH/c1-26-16(12(19)8-24-26)11-6-15(28-17(11)20)18(27)25-10(7-23)4-9-2-3-13(21)14(22)5-9;/h2-3,5-6,8,10H,4,7,23H2,1H3,(H,25,27);1H/t10-;/m0./s1
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| Chemical Name |
N-[(2S)-1-Amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide hydrochloride
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| Synonyms |
Afuresertib-F hydrochloride; Afuresertib-F; GSK2110183-analog; GSK-2110183-analog; GSK 2110183-analog; Afuresertib-F HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 90% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0757 mL | 10.3784 mL | 20.7568 mL | |
| 5 mM | 0.4151 mL | 2.0757 mL | 4.1514 mL | |
| 10 mM | 0.2076 mL | 1.0378 mL | 2.0757 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01445587 | Withdrawn | Drug: Part 1; Cohort 1 Drug: Part 1; Cohort 2 |
Cancer | GlaxoSmithKline | November 2011 | Phase 2 |
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