Serabelisib (TAK-117)

製品コードS8581 バッチS858101

印刷

化学情報

Synonyms

INK-1117, MLN-1117

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₉H₁₇N₅O₃

分子量

363.37

CAS No.

1268454-23-4

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

4 mg/mL (11.0 mM)

Water

Insoluble

Ethanol

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.2mg/ml (0.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	Serabelisib (TAK-117, INK-1117, MLN-1117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.
in vitro	Serabelisib (TAK-117) administration in PIK3CA-mutant tumor cell lines results in potent PI3K pathway inhibition, blockade of cellular proliferation, and apoptosis^[1]. It potently inhibits PI3K and demonstrates a greater than 100-fold selectivity relative to other class I PI3K family members and mTOR as well as a high degree of selectivity against a large panel of protein kinases. This compound blocks proliferation of tumor cell lines bearing PIK3CA mutations, and inhibits cellular phosphorylation and activity of AKT. However, it shows much less activity in PTEN-deficient tumor cells, which typically display constitutive PI3K pathway activation independent of PI3Kα^[3].
in vivo	Serabelisib (TAK-117) administration leads to dose-dependent inhibition of tumor growth in murine xenograft models of human cancer (e.g., breast carcinoma) bearing PIK3CA oncogenic mutations, with corresponding inhibition of PI3K pharmacodynamic markers in tumor tissue. Preclinical antitumor activity of this compound as a single agent has been shown to be independent of dosing schedules and driven by total plasma exposures. Conversely, it is not efficacious in tumor models harboring PTEN and/or KRAS mutations. Preclinical studies show TAK-117 to have low potential for disrupting glucose metabolism or for causing cardiac adverse events; in rats and monkeys, doses up to 50 mg/kg/day were well tolerated. In human, the mean terminal half-life is approximately 11 hours (range, 6-14 hours). There is no meaningful accumulation with repeated dosing for any schedule^[1]. Additionally, INK1117 does not significantly impair B and T cell function in vitro and in vivo^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NK cells
	濃度	20 min
	反応時間	1 μM
	実験の流れ	--
動物実験	動物モデル	C57BL/6 mice
	投薬量	60 mg/kg
	投与方法	oral

参考

https://pubmed.ncbi.nlm.nih.gov/28490463/
https://pubmed.ncbi.nlm.nih.gov/24915189/
http://mct.aacrjournals.org/content/10/11_Supplement/A171

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：

Enhancing immunotherapy through PD-L1 upregulation: the promising combination of anti-PD-L1 plus mTOR inhibitors [ Mol Oncol, 2025, 19(1):151-172]	PubMed: 39258533
Dihydroartemisinin alleviates skin fibrosis and endothelial dysfunction in bleomycin-induced skin fibrosis models [ Clin Rheumatol, 2021, 10.1007/s10067-021-05765-w]	PubMed: 34013490
Identification of Required Host Factors for SARS-CoV-2 Infection in Human Cells [ Cell, 2020, S0092-8674(20)31394-5]	PubMed: 33147445
In vivo microscopy reveals macrophage polarization locally promotes coherent microtubule dynamics in migrating cancer cells [ Nat Commun, 2020, 11(1):3521]	PubMed: 32665556

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。