AT13148
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205884

CAS#: 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.


Price and Availability

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Price

5mg
USD 150
50mg
USD 650
500mg
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Size
Price

10mg
USD 250
100mg
USD 950
1g
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Size
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25mg
USD 450
200mg
USD 1650
5g
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AT13148, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205884
Name: AT13148
CAS#: 1056901-62-2
Chemical Formula: C17H16ClN3O
Exact Mass: 313.09819
Molecular Weight: 313.78
Elemental Analysis: C, 65.07; H, 5.14; Cl, 11.30; N, 13.39; O, 5.10


Synonym: AT-13148; AT 13148; AT13148.

IUPAC/Chemical Name: (S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol

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


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

AT13148 is an orally active small molecule inhibitor of PKB/Akt and p70S6 kinase, key enzymes in the PI3K/PKB/mTOR tumor cell survival pathway. AT13148 has the potential to be a very effective inhibitor of AKT dependent tumors. In September 2008 Astex announced a partnership with Cancer Research UK and CRT to take AT13148 into development under the charity's Clinical Development Partnerships (CDP) program. Under the terms of this agreement, Cancer Research UK's Drug Development Office has carried out further development work on the agent, some of which is done in collaboration with the ICR. CRUK plans to commence phase 1 clinical trials of AT13148 at the Royal Marsden Hospital in the UK during 2012.  (source:http://astx.com/pipeline/products/clinical).
 
 
 


References

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.