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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- CAS No.: 2436473-55-9
- Formule: C27H31FN10O2
- Masse moléculaire:546.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
Chemical Information
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CAS No. 2436473-55-9
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Masse moléculaire 546.60
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RET-IN-4 Related Classifications
HY-132193 Related Classifications
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