2418533-90-9
Chemical Structure
VIP236
- CAS No.: 2418533-90-9
- Formula:C72H84N12Na2O20S
- Molecular Weight:1515.55
InChIKey: ZVBHCHRVKCGYDA-YBUSIOMQSA-L
SMILES: O=C(O[Na])C[C@@H](NC(NC1=CC=C(NC(NCCOCCOCCOCCC(N[C@H](C(N2[C@H](C(N[C@@H](C(C)C)C(O[C@@](C(OC3)=O)(CC)C4=C3C(N(CC5=C(CC)C(C=CC=C6)=C6N=C57)C7=C4)=O)=O)=O)CCC2)=O)CC(O[Na])=O)=O)=O)C=C1)=O)C8=CC=CC(NS(C9=CC=CC(NC(NCCC)=O)=C9)(=O)=O)=C8
Biological Activity: VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors[1][2][3][4].
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VIP236 | VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors. | |||||||||||||||||||||
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- [1]. Lerchen HG, et al. Discovery of VIP236, an αvβ3-Targeted Small-Molecule-Drug Conjugate with Neutrophil Elastase-Mediated Activation of 7-Ethyl Camptothecin Payload for Treatment of Solid Tumors. Cancers (Basel). 2023;15(17):4381. Published 2023 Sep 1. [Content Brief]
- [2]. Lerchen HG, et al. A Small Molecule-Drug Conjugate (SMDC) Consisting of a Modified Camptothecin Payload Linked to an αVß3 Binder for the Treatment of Multiple Cancer Types. Cancers (Basel). 2022;14(2):391. Published 2022 Jan 13. [Content Brief]
- [3]. Yang H, et al. Identification of an αvβ3-targeting bicyclic peptide with atypical norArg-Gly-Asp sequence. Commun Chem. 2026;9(1):83. Published 2026 Jan 12. [Content Brief]
Keywords