AT13148
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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

Size Price Shipping out time Quantity
10mg USD 90 Same Day
25mg USD 150 Same Day
50mg USD 250 Same Day
100mg USD 450 Same Day
200mg USD 750 Same Day
500mg USD 1650 Same Day
1g USD 2750 Same Day
2g USD 4250 Same Day
5g USD 6850 Same Day
Inquire bulk and customized quantity

Pricing updated 2020-10-20. Prices are subject to change without notice.

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


Related CAS #: 1056901-62-2   1056901-67-7 (R-isomer)   857532-13-9 (racemic)    

Synonym: AT-13148; AT 13148; AT13148; AT13148 hydrochloride; AT13148 HCl

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 (SDS):

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).

HS Tariff Code:
2934.99.9001


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.