YHO-13351 free base
Modify Date: 2024-01-03 17:06:45
YHO-13351 free base structure
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Common Name | YHO-13351 free base | ||
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| CAS Number | 912288-64-3 | Molecular Weight | 483.623 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 627.1±55.0 °C at 760 mmHg | |
| Molecular Formula | C26H33N3O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 333.1±31.5 °C | |
Use of YHO-13351 free baseYHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.IC50 value:Target: BCRP inhibitorin vitro: YHO-13177 potentiates the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38-resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the 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 [1].in vivo: In mice, YHO-13351 is rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increases 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 has little effect in these tumor models [1]. |
| Name | YHO-13351 free base |
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| Synonym | More Synonyms |
| Description | YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.IC50 value:Target: BCRP inhibitorin vitro: YHO-13177 potentiates the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38-resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the 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 [1].in vivo: In mice, YHO-13351 is rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increases 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 has little effect in these tumor models [1]. |
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| Related Catalog | |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 627.1±55.0 °C at 760 mmHg |
| Molecular Formula | C26H33N3O4S |
| Molecular Weight | 483.623 |
| Flash Point | 333.1±31.5 °C |
| Exact Mass | 483.219177 |
| LogP | 5.17 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.594 |
| Storage condition | 2-8℃ |
| 1-{5-[(Z)-2-Cyano-2-(3,4-dimethoxyphenyl)vinyl]-2-thienyl}-4-piperidinyl N,N-diethylglycinate |
| Glycine, N,N-diethyl-, 1-[5-[(Z)-2-cyano-2-(3,4-dimethoxyphenyl)ethenyl]-2-thienyl]-4-piperidinyl ester |
| YHO-13351 (free base) |