Structure
A-443654, inhibitor
A-443654
Purity
98.00%
Synonyms
A-443654; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 100mg/mL (251.59mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
(<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)
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].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for A-443654, inhibitor
A-443654 is a pan-Akt inhibitor. It has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
Product Categories/Family for A-443654, inhibitor
References
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.
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.
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Product Notes
The A-443654 (Catalog #AAA5754454) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "A-443654, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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