TAS-117 ( TAS117 )

Catalog No. M11679 CAS No. 1402602-94-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

TAS-117
Note

Research use only, not for human use.
Brief Description

TAS-117 is a highly selective, non-ATP competitive pan-Akt inhibitor with IC50 of 4.8/1.6/44 nM for Akt1/Akt2/Akt3 respectively.
Description

TAS-117 is a highly selective, non-ATP competitive pan-Akt inhibitor with IC50 of 4.8/1.6/44 nM for Akt1/Akt2/Akt3 respectively; shows minimal inhibitory activities against others kinases including PI3K, PDK1, and mTOR; inhibits Akt kinase activity but not p-Akt, blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1; induces significant cytotoxicity in MM cells associated with inhibition of IL6 secretion; triggers apoptosis and autophagy, induces ER stress response, inhibits human MM cell growth in murine xenograft models.Solid Tumors Phase 1 Clinical
Synonyms

TAS117
Pathway

Cytoskeleton/Cell Adhesion Molecules
Target

Akt
Recptor

Akt
Research Area

Cancer
Indication

Solid Tumors

CAS Number

1402602-94-1
Formula Weight

424.50
Molecular Formula

C26H24N4O2
Purity

>98% (HPLC)
Solubility

——
SMILES

C[C@]1(O)C[C@@](N)(C2=CC=C(C=C2)C3=C(C4=CC=CC=C4)N5COC6=CC=NC=C6C5=N3)C1
Chemical Name

Trans-3-amino-1methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-cyclobutanol

1. Mimura N, et al. Cancer Res. 2014 Aug 15;74(16):4458-69.
2. Koji Ichikawa, et al.

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