RET degrader-1
RET degrader-1 is a HyT degrader targeting RET. RET degrader-1 induces the degradation of CCDC6-RET via the ubiquitin-proteasome pathway. RET degrader-1 can be used in the research of RET-driven cancers.
(Pink: RET ligand (HY-149539); Blue: HyT ligand (HY-W013021); Black: linker (HY-76667)).
For research use only. We do not sell to patients.
- Formula: C33H37FN6O3
- Molecular Weight:584.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
RET degrader-1 (Compound B2) (1-10 μM; 48 h) achieves a 91.4% degradation rate of the CCDC6-RET fusion protein in TPC-1 cells, while the degradation rate observed at a concentration of 1 μM after 48 h of treatment is less than 20%[1].
RET degrader-1 (24-48 h) degrades GFP-tagged CCDC6-RET in transiently transfected HEK293T cells, as evidenced by the reduction in fluorescence intensity at 24 h and 48 h after treatment[1].
The degradation of the CCDC6-RET fusion protein in TPC-1 cells induced by RET degrader-1 is dependent on the ubiquitin-proteasome pathway, rather than the autophagy-lysosome pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human TPC-1 cells
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Concentration:1 μM, 10 μM
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Incubation Time:48 h
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Result:Reduced CCDC6-RET fusion protein levels by less than 20% at 1 μM for 48 h.
Reduced CCDC6-RET fusion protein levels by 91.4% at 10 μM for 48 h.
Confirmed a marked reduction in RET protein levels at 10 μM.
Chemical Information
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Molecular Weight 584.68
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Formula C33H37FN6O3
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SMILES
FC1=CC(/C2=C3\C(C4=C(C=CC=C4)N3)=N\OCCN(CC5)CCN5CCCNC(C6CC7CC6C=C7)=O)=C(C=C1)NC2=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)