DS-7423( DS7423 | DS 7423 )

Catalog No. M10844 CAS No. 1222104-37-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

DS-7423
Note

Research use only, not for human use.
Brief Description

DS-7423 is a novel potent, small-molecule dual inhibitor of PI3K/mTOR.
Description

DS-7423 is a novel potent, small-molecule dual inhibitor of PI3K/mTOR with IC50 of 15.6, 1143, 249, 262 and 34.9 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR? respectively; exerts anti-tumor effect against a panel of nine OCCA cell lines with IC50 of <75 nM, regardless of the mutational status of PIK3CA; suppresses the tumor growth of OCCA in a dose-dependent manner in mouse xenograft models.Solid Tumors Phase 1 Discontinued.
In Vitro

DS-7423 increases TP53 expression, the level of p-TP53 on Ser-46, and induced apoptosisrelated TP53 target genes (TP53AIP1 and PUMA) in OCCC cells.DS-7423 also inhibits other isoforms of class I PI3K (IC50 values: PI3Kβ = 1,143 nM; PI3Kγ = 249 nM; PI3Kδ = 262 nM).
In Vivo

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Synonyms

DS7423 | DS 7423
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

PI3K
Research Area

Cancer
Indication

Solid Tumors

CAS Number

1222104-37-1
Formula Weight

520.52
Molecular Formula

C22H27F3N10O2
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (192.12 mM)
SMILES

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Chemical Name

(R)-1-(4-(2-(2-aminopyrimidin-5-yl)-6-morpholino-9-(2,2,2-trifluoroethyl)-9H-purin-8-yl)-2-methylpiperazin-1-yl)ethan-1-one

1. Koul D, et al. Oncotarget. 2017 Mar 28;8(13):21741-21753. 2. Kashiyama T, et al. PLoS One. 2014 Feb 4;9(2):e87220.

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