YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific BCRP inhibitor.

YHO-13177 enhances SN-38, mitoxantrone and topotecan in BCRP transduced human colon cancer HCT116 (HCT116/BCRP) cells and BCRP-expressing SN-38 resistant human lung cancer A549 (A549/SN4) Cytotoxicity in cells, but little effect on parental cells. In addition, YHO-13177 potentiates the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. YHO-13177 increases the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppresses the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells .

YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration In mice. Coadministration of irinotecan with YHO-13351 significantly increased the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone had little effect in these tumor models .

1346753-00-1

C27H37N3O7S2

579.73

YHO-13351

DMSO:38 mg/mL (65.55 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years