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DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kα 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 PI3Kβ, 249 nM for PI3Kγ, and 262 nM for PI3Kδ[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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $129 | In Stock | |
5 mg | $297 | In Stock | |
10 mg | $455 | In Stock | |
25 mg | $745 | In Stock | |
50 mg | $987 | In Stock | |
100 mg | $1,450 | In Stock | |
1 mL x 10 mM (in DMSO) | $338 | In Stock |
Description | DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kα 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 PI3Kβ, 249 nM for PI3Kγ, and 262 nM for PI3Kδ[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. |
Targets&IC50 | PI3Kα:15.6 nM, mTOR:34.9 nM, PI3Kγ:249 nM, PI3Kβ:1143 nM, PI3Kδ:262 nM |
In vitro | DS-7423 elevates TP53 expression, enhances p-TP53 on Ser-46 phosphorylation, and stimulates apoptosis-related TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1]. Additionally, it selectively inhibits class I PI3K isoforms with varying IC50 values: PI3Kβ at 1,143 nM, PI3Kγ at 249 nM, and PI3Kδ at 262 nM[2]. |
Molecular Weight | 520.51 |
Formula | C22H27F3N10O2 |
Cas No. | 1222104-37-1 |
Smiles | C[C@@H]1CN(CCN1C(C)=O)c1nc2c(nc(nc2n1CC(F)(F)F)-c1cnc(N)nc1)N1CCOCC1 |
Relative Density. | 1.61 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 65 mg/mL (124.88 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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