YHO-13351
CAS No. : 1346753-00-1
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|---|---|---|
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| 10mg | $130 | In-stock |
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| Cat. No. : | HY-12758 |
| M.Wt: | 579.73 |
| Formula: | C27H37N3O7S2 |
| Purity: | >98 % |
| Solubility: | DMSO : 200 mg/mL (ultrasonic) |
YHO-13351 is an orally active ABCG2 inhibitor. YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer[1][2][3].
In Vitro:YHO-13351 (2 μM; 96 h) potently reverses SN-38 (HY-13704) resistance in ABCG2-overexpressing MDA-MB-231-S120 and NCI-N87-S120 cells, reducing the IC50 value of SN-38 by more than 90%[1].
YHO-13351 (0.004-0.1 μM) potently inhibits ABCG2-mediated Hoechst 33342 efflux in HeLa cells[3].
YHO-13351 (0.1 μg/mL; 96 h) sensitizes both HeLa SP cells and non-SP cells to SN-38 in vitro[3].
In Vivo:When administered in combination with IMMU-132 (HY-132254), YHO-13351 (0.6 mg; intravenous injection; single dose) increases the median survival time of mice bearing SN-38-resistant NCI-N87-S120 gastric cancer xenografts by 64% compared with untreated animals[1].
Combined with Irinotecan (HY-16562), YHO-13351 (100-200 mg/kg; i.p.; once daily on days 1, 5 and 9) dose-dependently prolongs the survival time of mice inoculated with P388/BCRP[2].
When used in combination with Irinotecan, YHO-13351 (30-200 mg/kg; p.o./i.v.; once daily on days 1, 5 and 9 / at 0 and 4 hours on days 1, 5 and 9 post-Irinotecan administration) dose-dependently enhances the antitumor activity of Irinotecan in HCT116/BCRP xenografts[2].
Combined with Irinotecan, YHO-13351 (600-1200 mg/kg; p.o.; administered on days 1, 5 and 9) inhibits tumor growth in HeLa non-SP cell and HeLa SP cell xenografts in nude mice[3].
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