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| Product | Description | |
|---|---|---|
| YHO-13351 | YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP. Synonyms: YHO-13351; YHO 13351; YHO13351. Grades: >98%. CAS No. 1346753-00-1. Molecular formula: C27H37N3O7S2. Mole weight: 579.73. |  |
| YHO-13351 free base | YHO-13351 free base is a potent and specific inhibitor of BCRP, which is the water-soluble prodrug of YHO-13177. It potentiates the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 cells and SN-38-resistant human lung cancer A549 cells, but had little effect in the parental cells in vitro. It also potentiates the cytotoxicity of SN-38 in human lung cancer NCI-H23 and NCI-H460, myeloma RPMI-8226 and pancreatic cancer AsPC-1 cell. It increases the intracellular accumulation of Hoechst 33342. It is rapidly converted into YHO-13177 after its oral or intravenous administration in mice. Uses: Yho-13351 free base could potentiate the cytotoxicity of sn-38, mitoxantrone and topotecan. Synonyms: YHO13351 free base; YHO 13351 free base; YHO-13351 free base. Grades: >98%. CAS No. 912288-64-3. Molecular formula: C26H33N3O4S. Mole weight: 483.62. | |
| BCRP Inhibitor IV, YHO-13351 (Diethylaminoacetic Acid, 1-(5-((Z)-2-cyano-2- (3, 4-dimethoxyphenyl) vinyl) thiophen-2-yl) piperidin-4-yl ester, Methanesulfonate) | An in vivo bioavailable (~87%; t1/2 <5 mins. during p.o. and i.v. administration) and highly water soluble (>100mg/ml) diethylaminoacetate prodrug of YHO-13177 that reverses BCRP-mediated irinotecan resistance in P388/BCRP and HCT116/BCRP xenograft mouse models, and suppresses tumor growth and significantly enhances the survival (100 or 200mg/kg, i.p.). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences. |  Worldwide |
| BCRP Inhibitor III, YHO-13177 ((Z)-2-(3,4-Dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile) | A cell-permeable acrylonitrile compound that potently inhibits breast cancer resistance protein (BCRP/ABCG2)-mediated drug export and reverses BCRP-mediated drug resistance in vitro (half maximal in the range 0.01-1uM) without altering the BCRP expression levels (in <6hrs.). Shown to selectively enable the intracellular accumulation of anticancer drugs and potentiate the cytotoxicity of BCRP-expressing carcinoma cells with no effect either on the P-glycoprotein/ABCB1- and MDRP1-mediated export or on the drug sensitivity of parental cells (IC50>10uM in A549 cells). An in vivo bioavailable and readily water soluble prodrug of YHO-13177, BCRP Inhibitor IV, YHO-13351 is also available. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
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