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616871-83-1

616871-83-1 Structure

616871-83-1 Structure
IdentificationBack Directory
[Name]

1,3-DIHYDRO-1-(1-((4-(6-PHENYL-1H-IMIDAZO[4,5-G]QUINOXALIN-7-YL)PHENYL)METHYL)-4-PIPERIDINYL)-2H-BENZIMIDAZOL-2-ONE TRIFLUOROACETATE SALT HYDRATE
[CAS]

NoCAS
[Synonyms]

AKT-I-1/2
AKT INHIBITOR VIII
AKT1/2 KINASE INHIBITOR
AKTI-1/2 TRIFLUOROACETATE SALT HYDRATE
AKT INHIBITOR VIII TRIFLUOROACETATE SALT HYDRATE
1,3-DIHYDRO-1-(1-((4-(6-PHENYL-1H-IMIDAZO[4,5-G]QUINOXALIN-7-YL)PHENYL)METHYL)-4-PIPERIDINYL)-2H-BENZIMIDAZOL-2-ONE TRIFLUOROACETATE SALT HYDRATE
Akt Inhibitor, Isozyme-selective (1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one
[Molecular Formula]

C36H32F3N7O4
[MDL Number]

MFCD08705407
[MOL File]

MFCD08705407
[Molecular Weight]

683.679
Chemical PropertiesBack Directory
[Melting point ]

>255oC (dec.)
[storage temp. ]

2-8°C
[solubility ]

DMSO (Slightly)
[form ]

powder
[color ]

yellow
[InChIKey]

CRRPFKCJZALCLQ-UHFFFAOYSA-N
[SMILES]

[H]O[H].OC(=O)C(F)(F)F.O=C1Nc2ccccc2N1C3CCN(CC3)Cc4ccc(cc4)-c5nc6cc7nc[nH]c7cc6nc5-c8ccccc8
Safety DataBack Directory
[WGK Germany ]

3
[Storage Class]

11 - Combustible Solids
Hazard InformationBack Directory
[Uses]

Akt plays a role in signal transduction pathways of cell proliferation, apoptosis, angiogenesis, and diabetes. Akt1 and Akt2 dual kinase inhibitors are capable of sensitizing tumor cells to certain apoptotic stimuli, and inhibit Akt phosphorylation in vivo. Akt1 kinase activity and its regulation by extracellular signaling factors in vivo in hematopoietic cells suggests the activation of AKT1 involves intracellular translocation of the kinase from cytosol to membrane.
[Biochem/physiol Actions]

Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.
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