2682939-53-1
Chemical Structure
Mal-Val-Ala-PAB(C2-glucuronic acid)-DMEA-PNU-159682
- CAS No.: 2682939-53-1
- Formula:C67H81N7O27
- Molecular Weight:1416.39
IUPAC Name: (2S,3S,4R,5R,6S)-6-(2-(4,7-dimethyl-3,8,11-trioxo-11-((2S,4S)-2,5,12-trihydroxy-7-methoxy-4-(((1S,3R,4aS,9S,9aR,10aS)-9-methoxy-1-methyloctahydro-1H-pyrano[4',3':4,5]oxazolo[2,3-c][1,4]oxazin-3-yl)oxy)-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-2-yl)-2,9-dioxa-4,7-diazaundecyl)-5-((S)-2-((S)-2-(2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)acetamido)-3-methylbutanamido)propanamido)phenethyl)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid
InChIKey: JBUOPLFZGFIWNV-MGFWFOFASA-N
SMILES: OC1=C2C(C(C(C(OC)=CC=C3)=C3C2=O)=O)=C(O)C4=C1C[C@](C(COC(N(C)CCN(C)C(OCC5=CC=C(NC([C@H](C)NC([C@H](C(C)C)NC(CN6C(C=CC6=O)=O)=O)=O)=O)C=C5CC[C@H]7[C@H](O)[C@@H](O)[C@H](O)[C@@H](C(O)=O)O7)=O)=O)=O)(O)C[C@@H]4O[C@H]8C[C@H](N(CCO[C@@H]9OC)[C@@H]9O%10)[C@H]%10[C@H](C)O8
Biological Activity: Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 is a drug-linker conjugate composed of a cleavable Val-Ala linker and the potent ADC cytotoxin PNU-159682 (HY-16700), which is applicable for ADC synthesis. When conjugated with an anti-CD46 antibody, Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 delivers its payload to CD46-expressing cells, while cathepsin B cleaves the Val-Ala linker to release the payload. ADCs synthesized from Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 drive durable responses in CD46-expressing patient-derived xenograft models of non-small cell lung cancer and colorectal cancer, and a single administration induces complete tumor regression in most models. Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 can be used in the research of non-small cell lung cancer and colorectal cancer[1].
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Mal-Val-Ala-PAB(C2-glucuronic acid)-DMEA-PNU-159682 | Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 is a drug-linker conjugate composed of a cleavable Val-Ala linker and the potent ADC cytotoxin PNU-159682 (HY-16700), which is applicable for ADC synthesis. When conjugated with an anti-CD46 antibody, Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 delivers its payload to CD46-expressing cells, while cathepsin B cleaves the Val-Ala linker to release the payload. ADCs synthesized from Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 drive durable responses in CD46-expressing patient-derived xenograft models of non-small cell lung cancer and colorectal cancer, and a single administration induces complete tumor regression in most models. Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 can be used in the research of non-small cell lung cancer and colorectal cancer. | |||||||||||||||||||||
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