CAIX/CAXII-IN prodrug-1 

CAIX/CAXII-IN prodrug-1 is a subtype-dependent prodrug inhibitor of carbonic anhydrase IX and XII (CAIX/CAXII). CAIX/CAXII-IN prodrug-1 itself shows no activity against carbonic anhydrases, and after hydrolysis, it exhibits K_i values of 54 nM and 62 nM against hCA IX and hCA XII, respectively. CAIX/CAXII-IN prodrug-1 exerts antiproliferative activity against cancer cells and induces cell apoptosis (apoptosis) via the endogenous mitochondrial pathway. CAIX/CAXII-IN prodrug-1 can be used in the research of breast cancer, colorectal adenocarcinoma and prostate cancer^[1].

CAIX/CAXII-IN prodrug-1 (Compound 10) (1 mM; 15 min-6 h) undergoes subtype-dependent phosphate ester hydrolysis, a process primarily mediated by recombinant human hCA IX and hCA XII, forming hydrolytic products after 6 h of incubation^[1].
CAIX/CAXII-IN prodrug-1 inhibits the proliferation of human MCF-7, MDA-MB-231, HCT116 and PC-3 cancer cell lines, with IC₅₀ values ranging from 16.1, 4.17, 2.02 to 1.83 μM, respectively, and exhibits the strongest activity against HCT116 and PC-3 cells^[1].
CAIX/CAXII-IN prodrug-1 (1.83 μM) activates the intrinsic mitochondrial apoptotic pathway in PC-3 cells by upregulating Bax, p53, caspase-3, caspase-9 and cytochrome c, while downregulating Bcl-2^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

226.17

C₁₀H₁₁O₄P

O=P1(OC)OC2=CC(OC)=CC=C2C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nocentini A, et al. Discovery of a Mixed and Prodrug-Like Inhibition Mechanism for Phosphocoumarins and Phosphoquinolinones against Human Carbonic Anhydrases. J Med Chem. 2026;69(9):11638-11648.