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Study on corrole photosensitizers (PSs) for photodynamic therapy (PDT) has made remarkable progress. Targeted delivery of PSs is of great significance for enhancing therapeutic efficiency, decreasing the dosage, and reducing systemic toxicity during PDT. The development of PSs that can be specifically delivered to the subcellular organelle is still an attractive and challenging work. Herein, we synthesize a series of azide-modified corrole phosphorus and gallium complex PSs, in which phosphorus corrole 2-P could not only precisely target the endoplasmic reticulum (ER) with a Pearson correlation coefficient (PCC) up to 0.92 but also possesses the highest singlet oxygen quantum yields (Φ Δ = 0.75). This renders it remarkable PDT activity at a very low dosage (IC 50 = 23 nM) towards HepG2 tumor cell line while ablating solid tumors in vivo with excellent biosecurity. Furthermore, 2-P exhibits intense red fluorescence (Φ F = 0.25), outstanding photostability, and a large Stokes shift (190 nm), making it a promising fluorescent probe for ER. This study provides a clinically potential photosensitizer for cancer photodynamic therapy and a promising ER fluorescent probe for bioimaging. A new kind of azide-modified corrole gallium (III) and phosphorus(V) complexes were synthesized and used as PDT photosensitizers. The prepared corrole phosphorus complex (2-P) can precisely target the endoplasmic reticulum (ER) and in situ generate massive reactive oxygen species (ROS) under irradiation to induce tumor regression at a very low dosage. [Display omitted] • Novel azide-modified corrole complexes for PDT were synthesized and evaluated. • 2-P could specifically target to endoplasmic reticulum. • 2-P could generate ROS and evoke mitochondria dysfunction upon PDT. • 2-P -mediated PDT could effectively eliminate tumor in vitro and in vivo. • 2-P -mediated PDT caused cell apoptosis in the caspase pathway. [ABSTRACT FROM AUTHOR]