2921735-91-1
Chemical Structure
APL-1092
Synonym(s): Mal-Exo-EEVC-Exatecan
- CAS No.: 2921735-91-1
- Formula:C65H77FN12O19
- Molecular Weight:1349.37
InChIKey: RNOMIXKVFJKKIV-UBDQZUTGSA-N
SMILES: O=C(C=CC1=O)N1CCCCCNC(C(C2=CC=C(C=C2)NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC([C@H](CCC(O)=O)NC([C@@H](NC(C)=O)CCC(O)=O)=O)=O)=O)=O)OC(N[C@@H]3C4=C5C(C(N6C5)=CC([C@](O)(C(OC7)=O)CC)=C7C6=O)=NC8=CC(F)=C(C)C(CC3)=C84)=O)=O
Biological Activity: APL-1092 is an EEVC linker-payload conjugate composed of exatecan, a stabilizer that prevents premature payload release, and a cleavage substrate for cathepsin B[1][2]. APL-1092 resists premature payload release mediated by human neutrophil elastase and carboxylesterase, maintains payload stability in mouse plasma, and retains cathepsin B-mediated cleavage activity in target cells[1]. APL-1092 exhibits dose-dependent tumor growth inhibition in xenograft mice[1]. APL-1092 can be used in gastric cancer-related research[1][2].
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APL-1092 | APL-1092 is an EEVC linker-payload conjugate composed of exatecan, a stabilizer that prevents premature payload release, and a cleavage substrate for cathepsin B. APL-1092 resists premature payload release mediated by human neutrophil elastase and carboxylesterase, maintains payload stability in mouse plasma, and retains cathepsin B-mediated cleavage activity in target cells. APL-1092 exhibits dose-dependent tumor growth inhibition in xenograft mice. APL-1092 can be used in gastric cancer-related research. | |||||||||||||||||||||
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- [1]. Watanabe T, et al. Exo-Cleavable Linkers: Enhanced Stability and Therapeutic Efficacy in Antibody-Drug Conjugates. Journal of medicinal chemistry. 2024 Oct 24;67(20):18124-18138. [Content Brief]
- [2]. Watanabe T, et al. Homogeneous Dual-Payload Antibody-Drug Conjugates Produced by Combined Distinct Conjugation Strategies. ACS medicinal chemistry letters. 2025 Jul 10;16(7):1334-1339. [Content Brief]
Keywords
