生物活性

Ridaifen-B (RID-B) is a novel tamoxifen (TAM) analog that significantly augments apoptosis-inducing effect of TAM in estrogen receptor (ER)-negatives cells. Ridaifen-B induces mitochondria-involved apoptosis in Jurkat cells, as evidenced by chromatin-condensed cells as well as downstream activation of caspases (caspase-3, -8 and -9) in a dose- and time-dependent manner. At 4 hours of incubation, IC50 for RID-B is 4 muM (30 muM for TAM). And at prolonged treatment of 48 hours, IC50 for RID-B is 0.1 muM.In a related reporton the global anti-tumor activity, RID-B strongly inhibits 39 human cancer cells (JFCR 39), both ER-+ or ER-- at concentrations of equal or less than 1muM (e.g., at 0.38muM for SF-539 [central nervous system], at 0.58muM for HT-29 [colon], at 0.20muM for DMS114 [lung], at 0.21muM for LOX-IMVI [melanoma], and at 0.23muM for MKN74 [stomach]. The binding protein of RID-B that exerts the apoptosis events is currently under investigation.

化学数据

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。