DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kalpha and mTOR, respectively, and exhibits anti-tumor activity[1][2]. It increases TP53 expression, the level of p-TP53 on Ser-46, and induces apoptosis-related TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1]. DS-7423 also inhibits other isoforms of class I PI3K with IC50 values of 1,143 nM for PI3Kbeta, 249 nM for PI3Kgamma, and 262 nM for PI3Kdelta[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul,42(7):757-62. [2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4,9(2):e87220.
Molekulargewicht:
520.51
Reinheit:
99.68%
CAS Nummer:
[1222104-37-1]
Formel:
C22H27F3N10O2
Target-Kategorie:
mTOR|||PI3K
T36083
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