Taletrectinib (DS-6051b)

製品コードS8901 バッチS890101

印刷

化学情報

Synonyms

AB-106

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₉H₃₄FN₅O₅

分子量

551.61

CAS No.

1505515-69-4

Solubility (25°C)*

体外

DMSO

50 mg/mL (90.64 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 Corn oil 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。	2.500mg/ml (4.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45%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。	5.000mg/ml (9.06mM)	Taking the 1 mL working solution as an example, add 100 μL of 50 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 450 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	タレクトレクチニブ（DS-6051b、AB-106）は、ROS1、TrkA、TrkB、TrkCに対するIC50値がそれぞれ0.207 nM、0.622 nM、2.28 nM、0.980 nMである、新世代の選択的ROS1/NTRK阻害剤です。
in vitro	Taletrectinib (DS-6051b) inhibited the growth of the CD74-ROS1 overexpressed Ba/F3 cells and the ROS1 fusion-positive HCC78 cancer cell line. It potently inhibited autophosphorylation of ROS1 in CD74-ROS1–expressed Ba/F3 cells and the SLC34A2-ROS1 harboring HCC78 cells at approximately single-digit to double-digit nanomolar concentration.
in vivo	In vivo experiments using the KM12-bearing mouse xenograft model shows that Taletrectinib (DS-6051b) induced tumor shrinkage at a ≥50 mg/kg or higher treatment dose without significant body weight loss.

プロトコル(参考用のみ)

参考

https://www.ncbi.nlm.nih.gov/pubmed/?term=The+new-generation+selective+ROS1%2FNTRK+inhibitor

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：

Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations [ Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025]	PubMed: 40299789
Novel insight into mechanisms of ROS1 catalytic activation via loss of the extracellular domain [ Sci Rep, 2024, 14(1):22191]	PubMed: 39333184
ADK-VR2, a cell line derived from a treatment-naïve patient with SDC4-ROS1 fusion-positive primarily crizotinib-resistant NSCLC: a novel preclinical model for new drug development of ROS1-rearranged NSCLC [ Transl Lung Cancer Res, 2022, 11(11:2216-2229)]	PubMed: 36519016
SHP2 Inhibition Enhances the Effects of Tyrosine Kinase Inhibitors in Preclinical Models of Treatment-naïve ALK-, ROS1-, or EGFR-altered Non-small Cell Lung Cancer [ Mol Cancer Ther, 2021, 20(9):1653-1662]	PubMed: 34158345
SHP2 inhibition enhances the effects of tyrosine kinase inhibitors in preclinical models of treatment-naïve ALK-, ROS1-, or EGFR-altered non-small-cell lung cancer [ Mol Cancer Ther, 2021, molcanther.0965.2020]	PubMed: 34158345
Mechanisms of targeted therapy resistance in a pediatric glioma driven by ETV6-NTRK3 fusion [ Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109]	PubMed: 34429303

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。