2682939-57-5
Chemical Structure
Mal-N(Me)-C6-N(Me)-PNU-159682
- CAS No.: 2682939-57-5
- Formula:C47H56N4O17
- Molecular Weight:948.96
InChIKey: DIKMHCCERKPKSJ-JDVHNQELSA-N
SMILES: OC1=C2C(C(C3=C(OC)C=CC=C3C2=O)=O)=C(O)C([C@H]4O[C@H]5C[C@]6([H])N7[C@]([C@H](OCC7)OC)([H])O[C@]6([H])[C@@H](O5)C)=C1C[C@](O)(C4)C(COC(N(C)CCCCCCN(C)C(CN8C(C=CC8=O)=O)=O)=O)=O
Biological Activity: Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC)[1].
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Mal-N(Me)-C6-N(Me)-PNU-159682 | Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC). | |||||||||||||||||||||
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