Rociletinib (CO-1686)

製品コードS7284 バッチS728402

印刷

化学情報

Chemical Structure Synonyms AVL-301 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C27H28F3N7O3
分子量 555.55 CAS No. 1374640-70-6
Solubility (25°C)* 体外 DMSO 100 mg/mL (180.0 mM)
Water Insoluble
Ethanol 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 Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.
in vitro CO-1686 inhibits p-EGFR with IC50 ranging from 62 to 187 nM in the mutant EGFR–expressing cells, while inhibits EGFR phosphorylation with IC50 of > 2,000 nM in the three WT EGFR–expressing cells. CO-1686 selectively inhibits growth of NSCLC cells expressing mutant EGFR with GI50 ranging from 7 to 32 nM, and induces apoptosis. CO-1686–resistant NSCLC cell lines exhibits signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors. [1]
in vivo CO-1686 causes dose-dependent and significant tumor growth inhibition in all EGFR-mutant models as well as human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Inhibition Kinetics Studies
Recombinant human wild-type and T790M/L858R double mutant EGFR, both Nterminal GST-tagged, are used in the assay. The Omnia continuous read assay is performed as described by the vendor.
細胞アッセイ 細胞株 NSCLC cell lines expressing mutant EGFR (HCC827, PC9, HCC827-EPR, and NCI-H1975) and cell lines expressing WT EGFR (A431, NCI-H1299, and NCI-H358)
濃度 ~10 μM
反応時間 72 hours
実験の流れ Cells are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.
動物実験 動物モデル Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
投薬量 ~50 mg/kg
投与方法 Oral gavage

カスタマーフィードバック

, , Cancer Res, 2017, 77(8):2078-2089

Data from [Data independently produced by , , Cancer Discov, 2015, 5(7): 713-22]

Data from [Data independently produced by , , Cancer Discov, 2015, 5(7): 713-22]

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：

Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] PubMed: 35118583
Targeting Aurora B kinase prevents and overcomes resistance to EGFR inhibitors in lung cancer by enhancing BIM- and PUMA-mediated apoptosis [ Cancer Cell, 2021, S1535-6108(21)00383-4] PubMed: 34388376
Overexpression of BIRC6 driven by EGF-JNK-HECTD1 signaling is a potential therapeutic target for triple-negative breast cancer [ Mol Ther Nucleic Acids, 2021, 26:798-812] PubMed: 34729249
Trametinib overcomes KRAS-G12V-induced osimertinib resistance in a leptomeningeal carcinomatosis model of EGFR-mutant lung cancer [ Cancer Sci, 2021, 112(9):3784-3795] PubMed: 34145930
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] PubMed: 34383271
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] PubMed: 34731453
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] PubMed: 34304386
Comprehensive pharmacogenomic characterization of gastric cancer. [ Genome Med, 2020, 18;12(1):17] PubMed: 32070411
Aspirin Sensitizes Osimertinib-Resistant NSCLC Cells in Vitro and in Vivo via Bim-dependent Apoptosis Induction [ Mol Oncol, 2020, 14(6):1152-1169] PubMed: 32239624

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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