Afuresertib NEW
| Price | $33 | $46 | $72 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Afuresertib | CAS No.: 1047644-62-1 |
| Purity: 99.17% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Afuresertib |
| Description | Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. |
| Cell Research | A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0-30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50's are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.(Only for Reference) |
| Kinase Assay | Potency (Ki*) of afuresertib: The true potency (Ki*) of the inhibitor is initially determined at low enzyme concentrations (0.1 nM AKT1, 0.7 nM AKT2, and 0.2 nM AKT3) using a filter binding assay and then confirmed with progress curve analysis. In the filter binding assay, a pre-mix of enzyme plus inhibitor is incubated for 1 h and then added to a GSKα peptide (Ac-KKGGRARTSS-FAEPG-amide) and [γ33P] ATP. Reactions are terminated after 2 h and the radio labeled AKT peptide product is captured in a phospho-cellulose filter plate. Progress curve analysis utilizes continuous real-time fluorescence detection of product formation using the Sox-AKT-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2). |
| In vitro | Overall 65% of hematological cell lines were sensitive to Afuresertib with an EC50 < 1 μM. 21% of solid tumor cell lines tested had an EC50 < 1 μM for Afuresertib. Afuresertib inhibited the kinase activity of the E17K AKT1 mutant protein with an EC50 of 0.2 nM. Afuresertib showed Afuresertib showed a concentration-dependent effect on the phosphorylation levels of multiple AKT substrates, including GSK3b, PRAS40, FOXO and cystatin 9. |
| In vivo | Overall 65% of hematological cell lines were sensitive to Afuresertib with an EC50 < 1 μM. 21% of solid tumor cell lines tested had an EC50 < 1 μM for Afuresertib. Afuresertib inhibited the kinase activity of the E17K AKT1 mutant protein with an EC50 of 0.2 nM. Afuresertib showed Afuresertib showed a concentration-dependent effect on the phosphorylation levels of multiple AKT substrates, including GSK3b, PRAS40, FOXO and cystatin 9. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (117.01 mM) Ethanol : 79 mg/mL (184.9 mM) |
| Keywords | ROK | Rho-associated kinase | Rho-kinase | Inhibitor | Rho-associated protein kinase | Akt | GSK-2110183 | inhibit | PKC | PKB | GSK 2110183 | Protein kinase C | Afuresertib | ROCK | Protein kinase B |
| Inhibitors Related | Ethyl gallate | Darovasertib | α-Vitamin E | Staurosporine | RKI-1447 | Artemisinin | Honokiol | Y-27632 dihydrochloride | Mitoxantrone dihydrochloride | 2,3-Butanediol | Y-27632 | Thiazovivin |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | TGF-beta/Smad Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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