AT7867 dihydrochloride NEW
| Price | $53 |
| Package | 2mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: AT7867 dihydrochloride | CAS No.: 1431697-86-7 |
| Supply Ability: 10g | Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | AT7867 dihydrochloride |
| Description | AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA kinase, with IC50 values of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively. It induces pharmacodynamic changes and inhibits human tumor xenograft growth. |
| In vitro | AT7867 ATP-competitive inhibited AKT2 with the Ki of 18nM. AT7867 also shows potent activity against the structurally related AGC kinases p70S6K and PKA, but shows a clear window of selectivity against kinases from other kinase sub-families. In vitro growth inhibition studies show that AT7867 blocks proliferation in a number of human cancer cell lines. AT7867 appears to be most potent at inhibiting proliferation in MES-SA uterine, MDA-MB-468 and MCF-7 breast, and HCT116 and HT29 colon lines (IC 50 values range from 0.9-3 μM), and least effective in the two prostate lines tested (IC 50 values range from 10-12 μM) [1]. |
| In vivo | After oral administration of AT7867 at a dosage of 20 mg/kg, its elimination from plasma mirrors that observed with intravenous (i.v.) administration. Plasma concentrations of AT7867 exceed 0.5 μM for a minimum of 6 hours post-oral dosing at 20 mg/kg. Based on the assumption of linear pharmacokinetics from i.v. administration, the oral bioavailability of AT7867 is estimated at 44%. Consequently, in vivo pharmacodynamic (PD) biomarker studies utilize this model. Subsequent to pharmacokinetic and tolerability assessments, AT7867 doses (90 mg/kg orally or 20 mg/kg intraperitoneally) are given to athymic mice harboring MES-SA tumors, with a focus on monitoring the phosphorylation levels of GSK3β and S6RP within the tumors over time. A significant reduction in the phosphorylation of these two pathway markers is observed at both 2 and 6 hours post-AT7867 administration. By the 24-hour mark, the total levels of GSK3β and S6RP have substantially decreased [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Keywords | AT 7867 | AT7867 | AT 7867 Dihydrochloride | AT-7867 Dihydrochloride | AT7867 dihydrochloride | AT7867 Dihydrochloride | AT-7867 |
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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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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