AdipoGen Life Sciences

A-674563 (free base)

CHF 55.00
In stock
AG-CR1-3680-M0011 mgCHF 55.00
AG-CR1-3680-M0055 mgCHF 190.00
AG-CR1-3680-M01010 mgCHF 270.00
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Product Details
Synonyms αS-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-benzeneethanamine
Product Type Chemical
Properties
Formula

C22H22N4O

MW 358.4
CAS 552325-73-2
Purity Chemicals ≥98% (HPLC)
Appearance Waxy solid.
Solubility Soluble in DMF (20mg/ml), DMSO (10mg/ml) or ethanol (10mg/ml).
InChi Key BPNUQXPIQBZCMR-IBGZPJMESA-N
Smiles CC1=NNC2=CC=C(C3=CC(OC[C@H](CC4=CC=CC=C4)N)=CN=C3)C=C21
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
Description
  • A-674563 is a potent, ATP-competitive, reversible and orally available Akt1 inhibitor with an IC50 of 11nM. Binds to the ATP site of the AKT kinase domain, inhibiting AKT-catalyzed phosphorylation activity.
  • Also inhibits PKA and CDK2 with IC50 values of 16nM and 46nM, respectively.
  • 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK and TK families.
  • Anticancer compound. Reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4µM.
  • Shown to decrease tumor growth in mouse tumor xenograft models.
  • Decreased sphingosine kinase 1 (SphK1) activity in AML cells to deplete pro-survival sphingosine-1-phosphate (S1P) and boost pro-apoptotic ceramide production.
Product References
  1. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo: Y. Luo, et al.; Mol. Cancer Ther. 4, 977 (2005)
  2. Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity: N. Rhodes, et al.; Cancer Res. 68, 2366 (2008)
  3. Soft tissue sarcoma cells are highly sensitive to AKT blockade: a role for p53-independent up-regulation of GADD45 alpha: Q.S. Zhu, et al.; Cancer Res. 68, 2895 (2008)
  4. Enhanced sensitivity to sorafenib by inhibition of Akt1 expression in human renal cell carcinoma ACHN cells both in vitro and in vivo: H. Tei, et al.; Hum. Cell. 28, 114 (2015)
  5. Unique roles of Akt1 and Akt2 in IGF-IR mediated lung tumorigenesis: S.E. Franks, et al.; Oncotarget 7, 3297 (2016)
  6. Dual inhibition of AKT/FLT3-ITD by A674563 overcomes FLT3 ligand-induced drug resistance in FLT3-ITD positive AML: A. Wang, et al.; Oncotarget 7, 29131 (2016)
  7. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells: L. Xu, et al.; BBRC 472, 662 (2016)
  8. Pre-clinical assessment of A-674563 as an anti-melanoma agent: Y. Zou, et al.; BBRC 477, 1 (2016)
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