Mubritinib, Free Base (1-[4-[4-[[2-[(1E)-2-[4-(Trifluoromethyl)phenyl]ethenyl]-4-oxazolyl]methoxy]ph

Mubritinib is a potent inhibitor of the human epidermal growth factor receptor 2 (HER2) tyrosine kinase. For inhibitory testing, HER2 was expressed in the following cell types: bladder (HT1376, UMUC3, T24), kidney (ACHN), and prostate (DU145, LNCaP, LN-REC4). IC50 values for mubritinib for the bladder cancer cell lines varied from 0.09 uM to greater than 25 uM. All of the prostate cancer cell lines studied were sensitive (IC50=0.053-4.6 uM) to mubritinib, but ACHN cells were relatively less sensitive. In the xenograft model, treatment with mubritinib for 14 days significantly inhibited growth of UMUC-3 (22.9%), ACHN (26.0%), and LN-REC4 (26.5%) when compared to control. Solubility: Soluble in DMSO at 25mg/ml with warming, soluble in ethanol at 1.7mg/ml, very poorly soluble in water, maximum solubility in plain water is estimated to be about 20-50uM, buffers, serum, or other additives may increase or decrease the aqueous solubility. Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.