VIP236 is a potent topoisomerase 1 inhibitor that selectively targets αvβ3 integrin for tumor localization. Upon binding, VIP236 leverages its cleavable linker, which is activated by neutrophil elastase prevalent in the tumor microenvironment, to deliver 7-ethylcamptothecin directly to cancer cells. This payload induces DNA damage through topoisomerase 1 inhibition, resulting in significant anti-tumor effects. VIP236 has demonstrated a 10-fold increased tumor/plasma ratio compared to traditional treatments, inducing tumor regression and reducing metastasis in various preclinical models, including non-small cell lung cancer, triple-negative breast cancer, and other metastatic solid tumors.
VIP236 is a potent topoisomerase 1 inhibitor that selectively targets αvβ3 integrin for tumor localization. Upon binding, VIP236 leverages its cleavable linker, which is activated by neutrophil elastase prevalent in the tumor microenvironment, to deliver 7-ethylcamptothecin directly to cancer cells. This payload induces DNA damage through topoisomerase 1 inhibition, resulting in significant anti-tumor effects. VIP236 has demonstrated a 10-fold increased tumor/plasma ratio compared to traditional treatments, inducing tumor regression and reducing metastasis in various preclinical models, including non-small cell lung cancer, triple-negative breast cancer, and other metastatic solid tumors.
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