Larotrectinib sulfate

製品コードS7960 バッチS796003

印刷

化学情報

Chemical Structure Synonyms LOXO-101 sulfate, ARRY-470 sulfate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H22F2N6O2.H2SO4
分子量 526.51 CAS No. 1223405-08-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (189.92 mM)
Ethanol 11 mg/mL (20.89 mM)
Water Insoluble
* <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 Larotrectinib sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.
in vitro ARRY-470(LOXO-101) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells[2].
in vivo Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Ba/F3 cells
濃度 10, 100, 1000 nM
反応時間 5 h
実験の流れ Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G, gefitinib 1,000 nM) or DMSO control. The cell lysate are used for western bolt analysis.
動物実験 動物モデル Adult male C3H/HeJ mice
投薬量 10-100 mg/kg
投与方法 p.o.

カスタマーフィードバック

Data from [Data independently produced by , , molecular cancer therapeutics]

Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(7):1526-1539]

Data from [Data independently produced by , , Analytical Biochemistry, 2018, 545(15):78-83]

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：

Generating in vitro models of NTRK-fusion mesenchymal neoplasia as tools for investigating kinase oncogenic activation and response to targeted therapy [ Oncogenesis, 2023, 12(1):8] PubMed: 36801905
Establishment and large-scale validation of a three-dimensional tumor model on an array chip for anticancer drug evaluation [ Front Pharmacol, 2022, 13:1032975] PubMed: 36313330
JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo [ Molecules, 2022, 27(19)6500] PubMed: 36235036
Influence of Tyrosine Kinase Inhibition on OATP1B3-mediated Uptake [ Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287] PubMed: 35383108
NTRK1/TrkA Activation Overrides the G2/M-Checkpoint upon Irradiation [ Cancers (Basel), 2021, 13(23)6023] PubMed: 34885133
Entrectinib Induces Apoptosis and Inhibits the Epithelial-Mesenchymal Transition in Gastric Cancer with NTRK Overexpression [ Int J Mol Sci, 2021, 23(1)395] PubMed: 35008821
NTRK Fusions Can Co-Occur With H3K27M Mutations and May Define Druggable Subclones Within Diffuse Midline Gliomas [ J Neuropathol Exp Neurol, 2021, nlab016] PubMed: 33749791
TRK inhibitors block NFKB and induce NRF2 in TRK fusion-positive colon cancer [ Journal of Cancer, 2021, 12(21): 6356-6362] PubMed: None
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
An Organoid Biobank of Neuroendocrine Neoplasms Enables Genotype-Phenotype Mapping [ Cell, 2020, 183(5):1420-1435.e21] PubMed: 33159857

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。