A-443654
| Code | Size | Price |
|---|
| AG-CR1-3663-M001 | 1 mg | £100.00 |
Quantity:
| AG-CR1-3663-M005 | 5 mg | £350.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Storage:
Short Term: +4°C. Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
(S)-1-(1H-Indol-3-yl)-3-((5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl)oxy)propan-2-amine
Appearance:
White to off-white solid.
CAS:
552325-16-3
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.Keep under inert gas.Protect from moisture and oxygen.
InChi:
InChI=1S/C24H23N5O/c1-15-22-10-16(6-7-24(22)29-28-15)17-9-20(13-26-11-17)30-14-19(25)8-18-12-27-23-5-3-2-4-21(18)23/h2-7,9-13,19,27H,8,14,25H2,1H3,(H,28,29)/t19-/m0/s1
InChiKey:
YWTBGJGMTBHQTM-IBGZPJMESA-N
Long Description:
Chemical. CAS: 552325-16-3. Formula: C24H23N5O. MW: 397.5. Synthetic. Potent and selective Akt inhibitor (Ki=160pmol/L for all three isoforms PKBalpha, PKBbeta and PKBgamma). 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.
MDL:
MFCD11840663
Molecular Formula:
C24H23N5O
Molecular Weight:
397.5
Package Type:
Plastic Vial
Product Description:
Potent and selective Akt inhibitor (Ki=160pmol/L for all three isoforms PKBalpha, PKBbeta and PKBgamma). 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.
Purity:
>98%
SMILES:
N[C@@H](CC1=CNC2=C1C=CC=C2)COC3=CC(C4=CC(C(C)=NN5)=C5C=C4)=CN=C3
Solubility Chemicals:
Soluble in DMSO (15mg/ml), ethanol (10mg/ml) or DMF (20mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo: L. Luo, et al.; Mol. Cancer Ther. 4, 977 (2005) | Akt inhibitor A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibition: E.K. Han, et al.; Oncogene 26, 5655 (2007) | 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) | The selectivity of protein kinase inhibitors: a further update: J. Bain, et al.; Biochem. J. 408, 297 (2007) | 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) | Akt inhibitor a-443654 interferes with mitotic progression by regulating aurora a kinase expression: X. Liu, et al.; Neoplasia 10, 828 (2008) | Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells: G.L. Gallia, et al.; Mol. Cancer Ther. 8, 386 (2009) | Akt inhibitors induce apoptosis in chronic lymphocytic leukemia cells: M. de Frias, et al.; Haematologica 94, 1698 (2009) | 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) | 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) | TORC2: a novel target for treating age-associated memory impairment: J.L. Johnson, et al.; Sci. Rep. 5, 15193 (2015)