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Akt &GSK-3

AT13148 (1056901-62-2)

AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity; AKT, p70S6K, PKA, ROCK, and SGK inhibitor.

Not Intended for Therapeutic Use. For research use only.

CAS: 1056901-62-2 Category

AT13148 (1056901-62-2) Description:

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.

AT13148 (1056901-62-2) Specifications:

Product Name AT13148
Synonym AT-13148; AT 13148; AT13148; AT13148 hydrochloride; AT13148 HCl
Chemical Name (S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1056901-62-2
Molecular Formula C17H16ClN3O
Molecular Weight 313.78
Monoisotopic Mass 313.09819 g/mol
MDL number MFCD25976789
InChIKey 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 ClC1=CC=C([[email protected]](C2=CC=C(C3=CNN=C3)C=C2)(O)CN)C=C1
Form Powder
Color White
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application AT13148 is an orally active small molecule inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. AT13148, a first-in-class multi-AGC kinase inhibitor, potently inhibits gastric cancer cells both in vitro and in vivo. Xi Y, Niu J, Shen Y, Li D, Peng X, Wu X. Biochem Biophys Res Commun. 2016 Sep 9;478(1):330-336. doi: 10.1016/j.bbrc.2016.01.167. Epub 2016 Jan 30. PMID: 26828267

[2]. Rho kinase inhibitors block melanoma cell migration and inhibit metastasis. Sadok A, McCarthy A, Caldwell J, Collins I, Garrett MD, Yeo M, Hooper S, Sahai E, Kuemper S, Mardakheh FK, Marshall CJ. Cancer Res. 2015 Jun 1;75(11):2272-84. doi: 10.1158/0008-5472.CAN-14-2156. Epub 2015 Apr 3. PMID: 25840982

[3]. Role of the anti-glioma drug AT13148 in the inhibition of Notch signaling pathway. Min W, Li Y, Zhang Y, Dai D, Cao Y, Yue Z, Liu J. Gene. 2015 Nov 15;573(1):153-9. doi: 10.1016/j.gene.2015.07.033. Epub 2015 Jul 15. PMID: 26187072

[4]. Rho Kinase Inhibition by AT13148 Blocks Pancreatic Ductal Adenocarcinoma Invasion and Tumor Growth. Rath N, Munro J, Cutiongco MF, Jagiełło A, Gadegaard N, McGarry L, Unbekandt M, Michalopoulou E, Kamphorst JJ, Sumpton D, Mackay G, Vennin C, Pajic M, Timpson P, Olson MF. Cancer Res. 2018 Jun 15;78(12):3321-3336. doi: 10.1158/0008-5472.CAN-17-1339. Epub 2018 Apr 18. PMID: 29669760

[5].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.

1 review for AT13148 (1056901-62-2)

  1. Cofttek

    Never had such good experience before,The AT13148 (1056901-62-2) is high purity,also customer service is pretty nice !gotta try!!

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