The invention discloses an ABPP-based antitumor drug ginsenoside Rg3 active molecular probe, synthesis and applications thereof, and belongs to the field of chemical biology. According to the presentinvention, the active molecular probe is designed and synthesized through structure modification based on the parent compound Rg3, can achieve the recognition and labeling of the drug action target inliving cells, has antitumor activity similar to Rg3, and provides the advantageous tool in the research on the antitumor action target and the action mechanisms of Rg3.