2412985-00-1
Chemical Structure
aTAG 4531
Synonym(s): CFT-4531
- CAS No.: 2412985-00-1
- Formula:C46H39F2N9O7
- Molecular Weight:867.85
InChIKey: BNHRIFMLKOQTPS-UHFFFAOYSA-N
SMILES: O=C(C1=C(F)C=C(C2=CC3=C(NC4=CC=CC=C4)C(C(NC5CC5)=O)=CN=C3C=C2F)C=C1)NCCCCN6N=NC(COC7=CC=CC(C(N8C9C(NC(CC9)=O)=O)=O)=C7C8=O)=C6
Biological Activity: aTAG 4531 is a PROTAC-class degrader that induces the degradation of the MTH1/aTAG fusion protein by recruiting cereblon, with a DC50 of 0.28 nM in Jurkat cells. aTAG 4531 inhibits MTH1 enzymatic activity, with a Ki of 1.8 nM. aTAG 4531 rapidly, selectively and reversibly regulates SMART-CAR protein levels, CAR-mediated target cell killing and IL-2 release, and is applicable both in vitro and in vivo. aTAG 4531 can be used in studies of targeted protein degradation, target validation and CAR-T activity regulation[1].
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aTAG 4531 | 99.1% | aTAG 4531 is a PROTAC-class degrader that induces the degradation of the MTH1/aTAG fusion protein by recruiting cereblon, with a DC50 of 0.28 nM in Jurkat cells. aTAG 4531 inhibits MTH1 enzymatic activity, with a Ki of 1.8 nM. aTAG 4531 rapidly, selectively and reversibly regulates SMART-CAR protein levels, CAR-mediated target cell killing and IL-2 release, and is applicable both in vitro and in vivo. aTAG 4531 can be used in studies of targeted protein degradation, target validation and CAR-T activity regulation. | ||||||||||||||||||||
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Keywords
