A-443654

CHF 120.00
In stock
AG-CR1-3663-M0011 mgCHF 120.00
AG-CR1-3663-M0055 mgCHF 440.00
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Product Details
Synonyms (S)-1-(1H-Indol-3-yl)-3-((5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl)oxy)propan-2-amine
Product Type Chemical
Properties
Formula C24H23N5O
MW 397.5
CAS 552325-16-3
Purity Chemicals ≥98%
Appearance White to off-white solid.
Solubility Soluble in DMSO (15mg/ml), ethanol (10mg/ml) or DMF (20mg/ml).
Identity Determined by 1H-NMR.
InChi Key YWTBGJGMTBHQTM-IBGZPJMESA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Keep under inert gas.
Protect from moisture and oxygen.
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
  • Potent and selective Akt inhibitor (Ki=160pmol/L for all three isoforms PKBα, PKBβ and PKBγ).
  • DYRK1A inhibitor (IC50=10nM). Inhibits other kinases, including PRK2, MSK1 and DYRK3 at low nM range as well.
  • Interferes with mitotic progression by regulating aurora a kinase expression and bipolar spindle formation. It induces G2/M accumulation, defects in centrosome separation and formation of either monopolar arrays or disorganized spindles.
  • Anticancer agent. Apoptosis inducer and chemosensitizing agent. Slows the progression and growth of Akt-dependent tumors.
  • Induces rapid Akt Ser473 phosphorylation independent of mTORC1 inhibition in human cancer cell lines.
  • Activates mTORC2 and reverses long-term memory deficits.
Product References
  1. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo: L. Luo, et al.; Mol. Cancer Ther. 4, 977 (2005)
  2. Akt inhibitor A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibition: E.K. Han, et al.; Oncogene 26, 5655 (2007)
  3. A role for Akt in epidermal growth factor-stimulated cell cycle progression in cultured hepatocytes: generation of a hyperproliferative window after adenoviral expression of constitutively active Akt: Y. Luo, et al.; J. Pharmacol. Exp. Ther. 321, 884 (2007)
  4. The selectivity of protein kinase inhibitors: a further update: J. Bain, et al.; Biochem. J. 408, 297 (2007)
  5. Proapoptotic activity and chemosensitizing effect of the novel Akt inhibitor (2S)-1-(1H-Indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan2-amine (A443654) in T-cell acute lymphoblastic leukemia: F. Fala, et al.; Mol. Pharmacol. 74, 884 (2008)
  6. Akt inhibitor a-443654 interferes with mitotic progression by regulating aurora a kinase expression: X. Liu, et al.; Neoplasia 10, 828 (2008)
  7. Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells: G.L. Gallia, et al.; Mol. Cancer Ther. 8, 386 (2009)
  8. Akt inhibitors induce apoptosis in chronic lymphocytic leukemia cells: M. de Frias, et al.; Haematologica 94, 1698 (2009)
  9. An allosteric Akt inhibitor effectively blocks Akt signaling and tumor growth with only transient effects on glucose and insulin levels in vivo: C. Cherrin, et al.; Cancer Biol. Ther. 9, 493 (2010)
  10. Recent Advances in the Design, Synthesis, and Biological Evaluation of Selective DYRK1A Inhibitors: A New Avenue for a Disease Modifying Treatment of Alzheimer's: B. Smith, et al.; ACS Chem. Neurosci. 3, 857 (2012)
  11. TORC2: a novel target for treating age-associated memory impairment: J.L. Johnson, et al.; Sci. Rep. 5, 15193 (2015)
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