受注:045-509-1970 |
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Synonyms | RXDX-101, NMS-E628 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C31H34F2N6O2 |
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分子量 | 560.64 | CAS No. | 1108743-60-7 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (178.36 mM) | |
Ethanol | 25 mg/mL (44.59 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. |
製品説明 | Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2. |
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in vitro | Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement. [2] |
in vivo | In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. [2] In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. [3] |
細胞アッセイ | 細胞株 | CUTO28 cells |
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濃度 | 12 nM | |
反応時間 | ||
実験の流れ | Cells were treated with different concentrations of entrectinib and proliferation was evaluated. |
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動物実験 | 動物モデル | Female NSG mice |
投薬量 | 50 mg/kg | |
投与方法 |
Data from [Data independently produced by , , Clin Cancer Res, 2018, 24(10):2357-2369]
Data from [Data independently produced by , , Clin Cancer Res, 2018, doi: 10.1158/1078-0432.CCR-17-1623]
Data from [Data independently produced by , , Cancer Med, 2017, 6(12):2972-2983]
Acquired NF2 mutation confers resistance to TRK inhibition in an ex vivo LMNA::NTRK1-rearranged soft-tissue sarcoma cell model [ J Pathol, 2024, 10.1002/path.6282] | PubMed: 38613194 |
The Combination of Afatinib With Dasatinib or Miransertib Results in Synergistic Growth Inhibition of Stomach Cancer Cells [ World J Oncol, 2024, 15(2):192-208] | PubMed: 38545471 |
NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations [ Cancer Discov, 2023, 13(3):598-615] | PubMed: 36511802 |
Discovery of oncogenic ROS1 missense mutations with sensitivity to tyrosine kinase inhibitors [ EMBO Mol Med, 2023, 10.15252/emmm.202217367] | PubMed: 37587872 |
Tyrosine Kinase Inhibitors Target B Lymphocytes [ Biomolecules, 2023, 13(3)438] | PubMed: 36979373 |
MET kinase inhibitor reverses resistance to entrectinib induced by hepatocyte growth factor in tumors with NTRK1 or ROS1 rearrangements [ Cancer Med, 2023, 12(5):5809-5820] | PubMed: 36416133 |
MET kinase inhibitor reverses resistance to entrectinib induced by hepatocyte growth factor in tumors with NTRK1 or ROS1 rearrangements [ Cancer Med, 2023, 12(5):5809-5820] | PubMed: 36416133 |
Inhibition of the epigenetically activated miR-483-5p/IGF-2 pathway results in rapid loss of meningioma tumor cell viability [ J Neurooncol, 2023, 162(1):109-118.] | PubMed: 36809604 |
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] | PubMed: 35868306 |
CIC-mediated modulation of MAPK signaling opposes receptor tyrosine kinase inhibitor response in kinase-addicted sarcoma [ Cancer Res, 2022, canres.1397.2021] | PubMed: 35074756 |
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。