2760847-82-1
Chemical Structure
PROTAC RET Degrader 1
- CAS No.: 2760847-82-1
- Formula:C48H57FN12O3
- Molecular Weight:869.04
InChIKey: CJWQEWFBJQOFIK-GUSHARESSA-N
SMILES: CCC1(CCN(CC1)C2=NC=C(C=C2)C3=NC(C4=CN(N=C4)[C@H]5CC[C@@H](CC5)N6CCC(CC6)C7=C(C=C(C=C7)NC8CCC(NC8=O)=O)F)=CN9N=CC(C#N)=C39)C(NC(C)C)=O
Biological Activity: PROTAC RET Degrader 1 is an orally active, blood-brain barrier-penetrant RET PROTAC degrader with a DC50 of 1.7 nM. PROTAC RET Degrader 1 binds to CRBN and forms a ternary complex with RET, mediating proteasomal degradation of RET, while also selectively mediating the degradation of SALL4. PROTAC RET Degrader 1 inhibits the RET signaling pathway, hERG channel activity, and Cyp3A4 enzyme activity; it suppresses cancer cell growth and induces tumor regression. PROTAC RET Degrader 1 can be used in research related to RET-driven cancers[1].
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PROTAC RET Degrader 1 | PROTAC RET Degrader 1 is an orally active, blood-brain barrier-penetrant RET PROTAC degrader with a DC50 of 1.7 nM. PROTAC RET Degrader 1 binds to CRBN and forms a ternary complex with RET, mediating proteasomal degradation of RET, while also selectively mediating the degradation of SALL4. PROTAC RET Degrader 1 inhibits the RET signaling pathway, hERG channel activity, and Cyp3A4 enzyme activity; it suppresses cancer cell growth and induces tumor regression. PROTAC RET Degrader 1 can be used in research related to RET-driven cancers. | |||||||||||||||||||||
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