Samotolisib (LY3023414)

製品コードS8322 バッチS832202

印刷

化学情報

Chemical Structure Synonyms GTPL8918 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H26N4O3
分子量 406.48 CAS No. 1386874-06-1
Solubility (25°C)* 体外 DMSO 81 mg/mL (199.27 mM)
Ethanol 40 mg/mL (98.4 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 LY3023414 (Samotolisib, GTPL8918) は、クラスI PI3Kアイソフォーム、mTOR、およびDNA-PKの経口ATP競合阻害剤です。
in vitro Samotolisib (LY3023414) shows high solubility across a wide pH range. In vitro, inhibition of PI3K/AKT/mTOR signaling by this compound causes G1 cell-cycle arrest and resulted in broad antiproliferative activity in cancer cell panel screens. In cell-based assays, its inhibition of PI3K and mTOR is assessed in the PTEN-deficient U87 MG glioblastoma cell line. It inhibits the phosphorylation of AKT at position T308 downstream of PI3K at an IC50 of 106 nM. Similarly, it inhibits phosphorylation of AKT at position S473 (IC50 = 94.2 nM) by mTORC2 as well as phosphorylation of mTORC1 kinase targets p70S6K (position T389; IC50 =10.6 nM) and 4E-BP1 (positions T37/46; IC50 = 187 nM). The downstream phosphorylation of S6RP at positions pS240/244 (IC50 = 19.1 nM) by p70S6K was inhibited as well, indicating target inhibition along the entire PI3K/AKT/mTOR pathway by this compound.
in vivo Samotolisib (LY3023414) demonstrates high bioavailability and dose-dependent dephosphorylation of PI3K/AKT/mTOR pathway downstream substrates such as AKT, S6K, S6RP, and 4E-BP1 for 4 to 6 hours in vivo, reflecting the drug's half-life of 2 hours. Intermittent target inhibition is sufficient for its antitumor activity. This compound shows time- and dose-dependent target inhibition in vivo. It is currently being evaluated in phase 1 and 2 trials for the treatment of human malignancies.

プロトコル(参考用のみ)

動物実験 動物モデル athymic nude, CD-1 nude and NMRI athymic nude mice(Xenograft tumors)
投薬量 --
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/27439478/

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2017, 8(58): 98964-98973]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Phosphorylation of PRAS40 contributes to the activation of the PI3K/AKT/mTOR signaling pathway and the inhibition of autophagy following status epilepticus in rats [ Experimental and Therapeutic Medicine, July 31, 2020, 3625-3632]
Targeting the PI3K/mTOR Pathway Augments CHK1 Inhibitor-Induced Replication Stress and Antitumor Activity in High-Grade Serous Ovarian Cancer [ Cancer Research, December 01, 2020, 5380-5392] PubMed: 32998994
LY3023414 inhibits both osteogenesis and osteoclastogenesis through the PI3K/Akt/GSK3 signalling pathway [ Bone & Joint Research, April 01, 2021, 237-249] PubMed: 33789427
Identification of nonsense-mediated decay inhibitors that alter the tumor immune landscape [ Elife, 2025, 13RP95952] PubMed: 39960487
Assessments of prostate cancer cell functions highlight differences between a pan-PI3K/mTOR inhibitor, gedatolisib, and single-node inhibitors of the PI3K/AKT/mTOR pathway [ Mol Oncol, 2024, 10.1002/1878-0261.13703] PubMed: 39092562
Functional Assessments of Gynecologic Cancer Models Highlight Differences Between Single-Node Inhibitors of the PI3K/AKT/mTOR Pathway and a Pan-PI3K/mTOR Inhibitor, Gedatolisib [ Cancers (Basel), 2024, 16(20)3520] PubMed: 39456616
Protective effect of leukemia inhibitory factor on the retinal injury induced by acute ocular hypertension in rats [ Exp Ther Med, 2023, 25(1):19] PubMed: 36561619
Research progress in molecular pathology markers in medulloblastoma [ Explor Target Antitumor Ther, 2023, 4(1):139-156] PubMed: 36937322
Functional impact and targetability of PI3KCA, GNAS, and PTEN mutations in a spindle cell rhabdomyosarcoma with MYOD1 L122R mutation [ Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140] PubMed: 35012940
Microenvironment drives cell state, plasticity, and drug response in pancreatic cancer [ Cell, 2021, 184(25):6119-6137.e26] PubMed: 34890551

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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