AT13148
AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors. AT13148 is currently being developed by Astex Pharmaceuticals. AT131148 was identified utilizing high-throughput X-ray crystallography and fragment-based lead discovery techniques. AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK and SGK substrate phosphorylation and induction of apoptosis in both a concentration and time-dependent manner in cancer cells with clinically relevant genetic defects both in vitro and in vivo.
1: Yap TA, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD. AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity. Clin Cancer Res. 2012 Jul 15;18(14):3912-23. doi: 10.1158/1078-0432.CCR-11-3313. Epub 2012 Jul 10. PubMed PMID: 22781553.
| Chemical | |
|---|---|
| CAS Num | 1056901-62-2 |
| Chemical Formula | C17H16ClN3O |
| Molecular Weight | 313.78 |
| IUPAC Chemical Name | (S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol |
| Exact Mass | 313.09819 |
| Elemental Analysis | C, 65.07; H, 5.14; Cl, 11.30; N, 13.39; O, 5.10 |
| Synonym | AT-13148; AT 13148; AT13148. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | ClC1=CC=C([C@](C2=CC=C(C3=CNN=C3)C=C2)(O)CN)C=C1 |
| Biological | |
| Targets and Effects | AKT inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | white solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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