RET-IN-4
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2436473-55-9
- 分子式: C27H31FN10O2
- 分子量:546.60
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
IC50: 1.29 nM (RET (WT)), 1.97 nM (RET (V804M)), and 0.99 nM (RET (M918T))[1]
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
19 nM
Compound: 9
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Antiproliferative activity against mouse KIF5B-RET BaF3 cells by cell based assay
Antiproliferative activity against mouse KIF5B-RET BaF3 cells by cell based assay
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[PMID: 34058344] |
The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion is effectively suppressed by RET-IN-4 (compound 9) (IC50 of 19 nM). RET-IN-4 displays less ‘off-target’ effects than BLU-667[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immunodeficient nude/nude mice bearing KIF5B-RET Ba/F3 cells[1]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:p.o.; daily; for 10 days
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Result:The tumor growth was remarkably suppressed.
化学情報
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CAS 番号 2436473-55-9
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分子量 546.60
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分子式 C27H31FN10O2
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SMILES
O=C1N([C@H](C2=CC=C(N3N=CC(F)=C3)N=C2)C)CCOC14CCN(C5=NC(NC6=NNC(C)=C6)=CC(C)=N5)CC4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
RET-IN-4 関連分類
HY-132193 関連分類
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