Description | YHO-13351 free base is a water-soluble prodrug of YHO-13177, an inhibitor of BCRP. |
In vivo | 在小鼠体内,口服或静脉注射YHO-13351后,该化合物迅速转化为YHO-13177。与YHO-13351联合给药的Irinotecan Hydrochloride显著延长了接种BCRP转导的小鼠白血病P388细胞的小鼠的生存时间,并有效抑制了HCT116/BCRP异种移植瘤模型中的肿瘤生长,而单独使用Irinotecan Hydrochloride在这些肿瘤模型中几乎没有效果[1]。 |
molecular weight | 483.62 |
Molecular formula | C26H33N3O4S |
CAS | 912288-64-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 90 mg/mL (186.1 mM), Sonication is recommended. |
References | 1. Yamazaki R, et al. Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. Mol Cancer Ther. 2011 Jul;10(7):1252-63. 2. Shishido Y, et al. ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Anticancer Res. 2013 Apr;33(4):1379-86. |