VIP236 is a small-molecule drug conjugate targeting alphavbeta3 integrin. VIP236 achieves tumor homing via specific binding to alphavbeta3 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].
Molecular Weight:
1515.55
CAS Number:
[2418533-90-9]
Formula:
C72H84N12Na2O20S
Target:
Elastase,Integrin
Application Notes:
MCE Product type: Reference compound
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