Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C24H23N5O |
Molecular Weight | 397.4723 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NNC2=CC=C(C=C12)C3=CC(OC[C@@H](N)CC4=CNC5=CC=CC=C45)=CN=C3
InChI
InChIKey=YWTBGJGMTBHQTM-IBGZPJMESA-N
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
Molecular Formula | C24H23N5O |
Molecular Weight | 397.4723 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/19465931 | https://www.ncbi.nlm.nih.gov/pubmed/18577685Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/19208828 | https://www.ncbi.nlm.nih.gov/pubmed/15956255
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19465931 | https://www.ncbi.nlm.nih.gov/pubmed/18577685
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/19208828 | https://www.ncbi.nlm.nih.gov/pubmed/15956255
A-443654 is a potent and selective AKT inhibitor. A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibition. A-443654 interferes with mitotic progression by regulating aurora a kinase expression. A-443654 inhibits all three Akt isoforms in FL5.12 cells stably transfected
with constitutively active myristoylated Akt1/2/3, and showed moderate selectivity when
screened against related kinases in the AGC family, such as PKA and PKC20. A-443654 has being shown to extend survival in an intracranial glioma animal model. A-443654, either alone or in combination with existing drugs, may be a useful therapy for primary and drug-resistant T-ALL.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15956255
Mice: A-443654 was given s.c. in a vehicle of 0.2% HPMC.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23470622
Treatment with A-443654 (0.5 uM), reduced FCS-stimulated growth of PA-SMCs (pulmonary artery smooth muscle cells) from MCT-PH rats to the level in control rats while inhibiting Akt, GSK3, and S6K activation.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 19:56:50 GMT 2023
by
admin
on
Sat Dec 16 19:56:50 GMT 2023
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Record UNII |
Q4UG565ZYH
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Record Status |
Validated (UNII)
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Record Version |
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552325-16-3
Created by
admin on Sat Dec 16 19:56:51 GMT 2023 , Edited by admin on Sat Dec 16 19:56:51 GMT 2023
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