名称 | DS-7423 |
描述 | 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. |
体外活性 | 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]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 65 mg/mL (124.88 mM)
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关键字 | mTOR | Phosphoinositide 3-kinase | Inhibitor | DS7423 | inhibit | PUMA | TP53 | Mammalian target of Rapamycin | PI3K | DS-7423 | OCCC | TP53AIP1 | DS 7423 |
相关产品 | L-Leucine | Capivasertib | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | Quercetin Dihydrate | Rapamycin | Apilimod |
相关库 | 糖酵解化合物库 | 经典已知活性库 | 激酶抑制剂库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌活性化合物库 | 抗癌药物库 |