MIP-1095

MIP-1095 (RPS-001) is a PSMA inhibitor with a K_i value of 0.24 nM. MIP-1095 binds to PSMA with high affinity and can be internalized into PSMA-expressing cancer cells. When radiolabeled with ¹²³I, ¹²⁴I or ¹³¹I, MIP-1095 enables SPECT/CT imaging, PET/CT imaging or targeted radiation delivery, respectively. ¹³¹I-MIP-1095 can alter serum PSA levels and relieve bone pain. MIP-1095 can be used in research related to metastatic castration-resistant prostate cancer^[1][2]. In Vitro:MIP-1095 (1-10000 nM; 30 minutes) potently inhibits the NAALADase activity of PSMA in human prostate cancer LNCaP cell lysates with a K_i of 0.24 nM^[1].
[¹²³I]MIP-1095 (3 nM; 1 hour) binds specifically to PSMA-positive human prostate cancer LNCaP cells but not to PSMA-negative human prostate cancer PC3 cells, with binding blocked by non-radiolabeled MIP-1095 or PMPA^[1].
[¹²³I]MIP-1095 (100 nM; 0-2 hour) undergoes time- and temperature-dependent internalization into human prostate cancer LNCaP cells via endocytosis^[1]. In Vivo:[¹²³I]MIP-1095 (1 mCi/mouse; i.v. tail vein) enables specific in vivo visualization of PSMA-expressing prostate cancer xenografts in mice via SPECT/CT imaging^[1].