RET-IN-36
RET-IN-36 is an orally active RET kinase inhibitor. RET-IN-36 overcomes gatekeeper and solvent front resistance mutations and inhibits the proliferation of cells expressing RETG810C and RETV804M mutants by suppressing RET phosphorylation and SHC downstream signaling. RET-IN-36 can be used for research on RET-mutant cancers, medullary thyroid cancer, papillary thyroid cancer, and non-small cell lung cancer.
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- Formule: C33H32FN7O2
- Masse moléculaire:577.65
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Stockage:
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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Activité biologique
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Chemical Information
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.0208 μM
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Antiproliferative activity against BaF3 cells stably expressing CCDC6-RETV804M assessed as reduction in cell proliferation incubated for 72 hrs by Cell Counting Kit 8 assay.
Antiproliferative activity against BaF3 cells stably expressing CCDC6-RETV804M assessed as reduction in cell proliferation incubated for 72 hrs by Cell Counting Kit 8 assay.
|
42607442 |
| BaF3 | IC50 |
0.096 μM
|
Antiproliferative activity against BaF3 cells stably expressing CCDC6-RETG810C assessed as reduction in cell proliferation incubated for 72 hrs by Cell Counting Kit 8 assay.
Antiproliferative activity against BaF3 cells stably expressing CCDC6-RETG810C assessed as reduction in cell proliferation incubated for 72 hrs by Cell Counting Kit 8 assay.
|
42607442 |
In Vitro
RET-IN-36 (3-300 nM; 6 h) inhibits RET signaling in BaF3-CCDC6-RETG810C cells[1].
RET-IN-36 (72 h) effectively inhibits the proliferation of BaF3 cells expressing CCDC6-RETV804M and CCDC6-RETG810C, with IC50 values of 0.0208 μM and 0.096 μM, respectively[1].
RET-IN-36 (0.3 μM; 6 h) dose-dependently inhibits RET activation and downstream signaling through SHC in BaF3-CCDC6-RETG810C cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BaF3-CCDC6-RETG810C cells
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Concentration:3, 10, 30, 100, 300 nM
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Incubation Time:6 h
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Result:Inhibited RET signaling in BaF3-CCDC6-RETG810C cells.
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Cell Line:BaF3 cells expressing CCDC6-RETG810C
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Concentration:0.3 μM
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Incubation Time:6 h
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Result:Inhibited RET phosphorylation and downstream signaling through SHC at 0.3 μM.
Parmacokinetics
Chemical Information
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Masse moléculaire 577.65
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Formule C33H32FN7O2
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SMILES
FC1=C(N2C=CC(NC3=NC(N([C@@H]4CCCN(C(C5CC5)=O)C4)C(C(C6=C(C)C=CC=C6)=C7C)=O)=C7C=N3)=N2)C=CC=C1
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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-36 Related Classifications
HY-189268 Related Classifications
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