RET-IN-32
RET-IN-32 is an orally active RET inhibitor with IC50 values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer.
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- No. CAS: 2620629-32-3
- Fòrmula: C33H35N7O4
- Peso molecular:593.68
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
RET-IN-32 (Compound 9) (72 h) inhibits the proliferation of BAF3-KIF5B-RET-WT cells with an IC50 of 1.2 nM; it also inhibits the proliferation of BAF3-KIF5B-RETV804M cells with an IC50 of 212 nM[1].
RET-IN-32 (1-100 nM; 12 h) reduces the mRNA expression of SPRY4 and DUSP6 in a dose-dependent manner in BAF3-KIF5B-RET-WT cells, but has no effect on the mRNA expression of GSK3B[1].
RET-IN-32 (1-1000 nM; 1 h) significantly inhibits autophosphorylation of RET Tyr1062 in BAF3-KIF5B-RET-WT cells at a concentration of 10 nM, and achieves almost complete inhibition at 100 nM[1].
RET-IN-32 (1-1000 nM; 12 h) induces dose-dependent G0/G1 phase arrest and reduces the S-phase cell population in BAF3-KIF5B-RET-WT cells[1].
RET-IN-32 (10-1000 nM; 12 h) induces apoptosis in BAF3-KIF5B-RET-WT cells at concentrations of 100 nM and 1000 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BAF3-KIF5B-RET-WT cells
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Concentration:1, 10 and 100 nM
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Incubation Time:12 h
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Result:Exhibited dose-dependent inhibition of SPRY4 and DUSP6 mRNA expression.
Had no effect on GSK3B mRNA expression.
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Cell Line:BAF3-KIF5B-RET-WT cells
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Concentration:1, 10, 100 and 1000 nM
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Incubation Time:1 h
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Result:Significantly inhibited RET autophosphorylation on Tyr1062 at 10 nM.
Nearly completely inhibited RET autophosphorylation at 100 nM.
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Cell Line:BAF3-KIF5B-RET-WT cells
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Concentration:1, 10, 100 and 1000 nM
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Incubation Time:12 h
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Result:Induced dose-dependent G0/G1 phase arrest in BAF3-KIF5B-RET-WT cells.
Inhibited S phase progression in BAF3-KIF5B-RET-WT cells.
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Cell Line:BAF3-KIF5B-RET-WT cells
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Concentration:1, 10, 100 and 1000 nM
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Incubation Time:12 h
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Result:Increased the fraction of apoptotic cells in BAF3-KIF5B-RET-WT cells at 100 nM dose compared to the blank control group.
Increased the fraction of apoptotic cells in BAF3-KIF5B-RET-WT cells at 1000 nM dose compared to the blank control group.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude (male, 4-6 weeks old, 18-20 g, subcutaneous xenograft model)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.g.; twice daily; 15 days
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Result:Produced significant dose-dependent reductions in tumor weight compared to vehicle control.
Achieved complete tumor growth inhibition at 10 mg/kg dose.
Caused no mortality or body weight changes in any treatment group throughout the 15-day study.
Chemical Information
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No. CAS 2620629-32-3
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Peso molecular 593.68
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Fòrmula C33H35N7O4
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SMILES
COC1=NC=C(C=C1)CN2C3CC2CN(C3)C4=NC=C(C=C4)C5=CC(OCCOC6CC7(C6)COC7)=CN8N=CC(C#N)=C58
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RET-IN-32 Related Classifications
HY-182741 Related Classifications
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