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A-443654 Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5754454

A-443654 is a pan-Akt inhibitor. It has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
A-443654, Inhibitor
Full Product Name
A-443654
Product Gene Name
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
397.47
Solubility
DMSO: 100mg/mL (251.59mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C24H23N5O
SMILES
N[C@H](COC1=CN=CC(C2=CC3=C(NN=C3C)C=C2)=C1)CC4=CNC5=CC=CC=C54
CAS Number
552325-16-3
Target & IC50
Akt1: ic50 160pM (ki)
Akt2: ic50 160pM (ki)
Akt3: ic50 160pM (ki)
PKA: ic50 6.3nM (ki)
RSK2: ic50 11nM (ki)
PKCgamma: ic50 24nM (ki)
CDK2: ic50 24nM (ki)
PKCdelta: ic50 33nM (ki)
GSK3beta: ic50 41nM (ki)
ERK2: ic50 340nM (ki)
cKIT: ic50 1.2uM (ki)
Chk1: ic50 2.3uM (ki)
CK2: ic50 2.4uM (ki)
SRC: ic50 2.6uM (ki)
KDR: ic50 3.1uM (ki)
MAPK-AP2: ic50 3.3uM (ki)
Flt1: ic50 3.6uM (ki)
In Vitro
A-443654 (7.5mg/kg/d, s.c.) inhibits tumor growth in the 3T3-Akt1 flank tumor model. A-443654 (50mg/kg, s.c.) induces apoptosis in 3T3-Akt1 flank tumors. A-443654 (30mg/kg, s.c.) leads to increased levels of phosphorylated Akt1 in MiaPaCa-2 tumors[1].

Structure of A-443654, inhibitor

A-443654 Inhibitor – Cat# MBS5754454

Product References and Citations for A-443654, inhibitor

Luo Y, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005 Jun;4(6):977-86.
Luo Y, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005 Jun;4(6):977-86.
Zheng J, et al. Rapamycin sensitizes Akt inhibition in malignant human breast epithelial cells. Cancer Lett. 2010 Oct 1;296(1):74-87.
Zheng J, et al. Rapamycin sensitizes Akt inhibition in malignant human breast epithelial cells. Cancer Lett. 2010 Oct 1;296(1):74-87.
Gallia GL, et al. Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells. Mol Cancer Ther. 2009 Feb;8(2):386-93.
Gallia GL, et al. Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells. Mol Cancer Ther. 2009 Feb;8(2):386-93.
Zhao Y, et al. Estrogen receptor alpha and beta regulate actin polymerization and spatial memory through an SRC-1/mTORC2-dependent pathway in the hippocampus of female mice. J Steroid Biochem Mol Biol. 2017 Nov;174:96-113.
Zhao Y, et al. Estrogen receptor alpha and beta regulate actin polymerization and spatial memory through an SRC-1/mTORC2-dependent pathway in the hippocampus of female mice. J Steroid Biochem Mol Biol. 2017 Nov;174:96-113.

Other Notes

Small volumes of A-443654, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for A-443654 purchase

MBS5754454 is an inhibitor targeting A-443654.
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