product name AT13148
Description: AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. In vitro studies, AT13148 has been reported to inhibit activity of AGC kinases which including AKT, p70S6 kinase, PKA, SGK and Rho kinase with the IC50 values of 38nM, 8nM, 3nM, 63nM and 4nM, respectively. In addition, AT13148 has been revealed to inhibit proliferation with GI50 values of 1.54μM, 1.59μM, 1.82μM, 2.65μM and 3.77μM in MES-SA, BT474, HCT-116, A549 and SK-OV-3 cell lines, respectively.
References: Clin Cancer Res. 2012 Jul 15;18(14):3912-23.
313.78
Formula
C17H16ClN3O
CAS No.
1056901-62-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 62 mg/mL (197.59 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Chemical Name
(S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394480
| In Vitro | Kinase Assay: AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.
Cell Assay: Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. Cell lines: MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines; Incubation Time: 72 hours or 96 hours AT13148, as a multi-AGC kinase inhibitor, potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K signaling. |
|---|---|
| In Vivo | AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and p70S6K AGC kinases, and subsequently exhibits marked antitumor effects in human tumor xenografts. |
| Animal model | Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts |
| Formulation & Dosage | Dissolved in 10% DMSO, 1% Tween-20, and 89% saline; 50 mg/kg; p.o. |
| References | [1] Yap TA, et al. Clin Cancer Res. 2012, 18(14), 3912-3923. |
Related Posts
product name AT13148
Description: AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. In vitro studies, AT13148 has been reported to inhibit activity of AGC kinases which including AKT, p70S6 kinase, PKA, SGK and Rho kinase with the IC50 values of 38nM, 8nM, 3nM, 63nM and 4nM, respectively. In addition, AT13148 has been revealed to inhibit proliferation with GI50 values of 1.54μM, 1.59μM, 1.82μM, 2.65μM and 3.77μM in MES-SA, BT474, HCT-116, A549 and SK-OV-3 cell lines, respectively.
References: Clin Cancer Res. 2012 Jul 15;18(14):3912-23.
313.78
Formula
C17H16ClN3O
CAS No.
1056901-62-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 62 mg/mL (197.59 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Chemical Name
(S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394480
| In Vitro | Kinase Assay: AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.
Cell Assay: Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. Cell lines: MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines; Incubation Time: 72 hours or 96 hours AT13148, as a multi-AGC kinase inhibitor, potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K signaling. |
|---|---|
| In Vivo | AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and p70S6K AGC kinases, and subsequently exhibits marked antitumor effects in human tumor xenografts. |
| Animal model | Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts |
| Formulation & Dosage | Dissolved in 10% DMSO, 1% Tween-20, and 89% saline; 50 mg/kg; p.o. |
| References | [1] Yap TA, et al. Clin Cancer Res. 2012, 18(14), 3912-3923. |