RD-23
RD-23 is an orally active and selective RET PROTAC degrader, with DC50 values of 5.6 nM and 11.7 nM against RETWT and RETG810C mutants, respectively. RD-23 inhibits purified RET kinase activity with an IC50 of 0.371 nM. RD-23 suppresses the activation of downstream Shc signaling and induces apoptosis. RD-23 can be used for the research of RET-related cancers.
(Pink: RET ligand (HY-168868); Blue: Cereblon ligand (HY-43722); Black: linker (HY-W010642)).
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- No. CAS: 3053537-06-4
- Fòrmula: C52H56N12O4
- Peso molecular:913.08
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
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Cereblon |
RD-23 potently inhibits the proliferation of Ba/F3-KIF5B-RET cells with an IC50 of 2.6 nM[1].
RD-23 potently inhibits the proliferation of Ba/F3-KIF5B-RETV804M cells with an IC50 of 5.2 nM[1].
RD-23 potently inhibits the proliferation of Ba/F3-KIF5B-RETG810C cells with an IC50 of 5.3 nM[1].
RD-23 inhibits the proliferation of Ba/F3-KIF5B-RETG810R cells with an IC50 of 165.2 nM[1].
RD-23 inhibits the proliferation of Ba/F3-KIF5B-RETG810S cells with an IC50 of 22.6 nM[1].
RD-23 potently inhibits the proliferation of Ba/F3-CCDC6-RET cells with an IC50 of 2.4 nM[1].
RD-23 potently inhibits the proliferation of Ba/F3-CCDC6-RETV804M cells with an IC50 of 4.5 nM[1].
RD-23 potently inhibits the proliferation of Ba/F3-CCDC6-RETG810C cells with an IC50 of 6.5 nM[1].
RD-23 inhibits the proliferation of Ba/F3-CCDC6-RETG810R cells with an IC50 of 121.5 nM[1].
RD-23 (1-50 nM; 24 h) inhibits downstream Shc activation in a concentration-dependent manner in Ba/F3-KIF5B-RETG810C cells after 24 h of treatment[1].
RD-23 (10-40 nM; 48 h) induces dose-dependent apoptosis in Ba/F3-KIF5B-RETG810C cells after 48 h of treatment, with 71.3% of cells apoptotic at a concentration of 40 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3-KIF5B-RETG810C
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Concentration:1, 10, 20 and 50 nM
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Incubation Time:24 h
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Result:Inhibited activation of downstream Shc signaling in a concentration-dependent manner, with reduced levels of phosphorylated Shc corresponding to reduced RET protein levels.
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Cell Line:Ba/F3-KIF5B-RETG810C
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Concentration:10, 20 and 40 nM
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Incubation Time:48 h
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Result:Induced dose-dependent apoptosis, with apoptotic cell percentages reaching 34.1% (10 nM), 55.4% (20 nM), and 71.3% (40 nM), which were significantly higher than the control group's 6.7%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nu/nu (female, 6 to 8 weeks old, subcutaneously implanted with 5 × 106 Ba/F3-KIF5B-RETG810C cells)[1]
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Dosage:10 mg/kg
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Administration:p.o.; once or twice daily; 10 days
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Result:Induced 62.3% tumor growth inhibition at 10 mg/kg p.o. once daily.
Induced 85.1% tumor growth inhibition at 10 mg/kg p.o. twice daily.
Induced degradation of the RET protein in tumor tissue.
Did not cause significant body weight changes during treatment.
Chemical Information
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No. CAS 3053537-06-4
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Peso molecular 913.08
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Fòrmula C52H56N12O4
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SMILES
N#CC1=C2C(C3=CC=C(N=C3)N4CC5CC(C4)N5CC6=CC=C(N=C6)OC)=CC(N7CCC(CC7)N8CCN(CC8)CCCC#CC9=CC=CC%10=C9CN(C%10=O)C(C(N%11)=O)CCC%11=O)=CN2N=C1
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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)
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