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Akt &GSK-3

A-674563 (552325-73-2)

A-674563 is a potent, orally available Akt1 inhibitor with an IC50 value of 11nM. Also displays activity against PKA and CDK2 with IC50 values of 16nM and 46nM respectively….

Not Intended for Therapeutic Use. For research use only.

CAS: 552325-73-2 Category

A-674563 (552325-73-2) Description:

The present study aims to investigate the anti-melanoma activity by an Akt1 specific inhibitor A-674563. We showed that A-674563 was anti-proliferative and cytotoxic when added to human melanoma cells (A375, WM-115 and SK-Mel-2 lines). A-674563 induced caspase-dependent apoptotic death of human melanoma cells, and its cytotoxicity was inhibited with pre-treatment of caspase inhibitors.

A-674563 (552325-73-2) Specifications:

Product Name A-674563
Synonym A674563; A 674563; A-674563
Chemical Name (S)-1-((5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl)oxy)-3-phenylpropan-2-amine
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 552325-73-2
Molecular Formula C22H22N4O
Molecular Weight 358.43628
Monoisotopic Mass 358.17936 g/mol
MDL number N/A
InChIKey BPNUQXPIQBZCMR-IBGZPJMESA-N
InChi Code InChI=1S/C22H22N4O/c1-15-21-11-17(7-8-22(21)26-25-15)18-10-20(13-24-12-18)27-14-19(23)9-16-5-3-2-4-6-16/h2-8,10-13,19H,9,14,23H2,1H3,(H,25,26)/t19-/m0/s1
SMILES N[[email protected]@H](CC1=CC=CC=C1)COC2=CC(C3=CC4=C(NN=C4C)C=C3)=CN=C2
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 >5 years if stored properly
Handling Protect from air and moisture
Application A-674563 is a potent, orally available Akt1 inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Tei H, Miyake H, Fujisawa M. Enhanced sensitivity to sorafenib by inhibition of Akt1 expression in human renal cell carcinoma ACHN cells both in vitro and in vivo. Hum Cell. 2015 Apr 11. [Epub ahead of print] PubMed PMID: 25862630.

[2]. A-674563 increases chondrocyte marker expression in cultured chondrocytes by inhibiting Sox9 degradation. Kobayashi T, Fujita K, Kamatani T, Matsuda S, Tsumaki N. Biochem Biophys Res Commun. 2018 Jan 1;495(1):1468-1475. doi: 10.1016/j.bbrc.2017.11.180. Epub 2017 Dec 5. PMID: 29196261

[3]. Pre-clinical assessment of A-674563 as an anti-melanoma agent. Zou Y, Fan G, Wang X. Biochem Biophys Res Commun. 2016 Aug 12;477(1):1-8. doi: 10.1016/j.bbrc.2016.03.020. Epub 2016 Mar 10. PMID: 26970307

[4]. A-674563, a putative AKT1 inhibitor that also suppresses CDK2 activity, inhibits human NSCLC cell growth more effectively than the pan-AKT inhibitor, MK-2206. Chorner PM, Moorehead RA. PLoS One. 2018 Feb 22;13(2):e0193344. doi: 10.1371/journal.pone.0193344. eCollection 2018. PMID: 29470540

[5].Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells. Xu L, Zhang Y, Gao M, Wang G, Fu Y. Biochem Biophys Res Commun. 2016 Apr 15;472(4):662-8. doi: 10.1016/j.bbrc.2016.02.094. Epub 2016 Feb 23. PMID: 26920060

1 review for A-674563 (552325-73-2)

  1. Cofttek

    Never had such good experience before,The A-674563 (552325-73-2) is high purity,also customer service is pretty nice !gotta try!!

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