| CAS NO: | 1056901-62-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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 | |
| Other info | Synonym: AT-13148; AT 13148; AT13148; AT13148 hydrochloride; AT13148 HCl InChi Key: IIRWNGPLJQXWFJ-KRWDZBQOSA-N InChi Code: InChI=1S/C17H16ClN3O/c18-16-7-5-15(6-8-16)17(22,11-19)14-3-1-12(2-4-14)13-9-20-21-10-13/h1-10,22H,11,19H2,(H,20,21)/t17-/m0/s1 SMILES Code: ClC1=CC=C([C@](C2=CC=C(C3=CNN=C3)C=C2)(O)CN)C=C1 |
| Chemical Name | (S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol |
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. |
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