AZD3759？AZD3759 is an oral inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor activating mutations with the following activity in cell-based proliferation assays: Inhibition of tumour cell proliferation: anti-proliferative activity in EGFRm+ cell lines with pEGFR IC50 of 0.007 µM. In contrast, AZD3759 displayed much less potent anti-proliferative activity across a number of cell lines with wild type EGFRs, with pEGFR IC50 of 0.065 µM. Inhibition of signalling in subcutaneous xenograft models: AZD3759 dosed orally once daily induced tumour regression in a dose-dependent manner in EGFRm+ xenograft model (starting from 3.75mg/kg qd), but did not induce tumour regression in EGFR wild type xenograft model. In addition, AZD3759 led to tumour regression in EGFRm+ brain metastasis (BM) and leptomeningeal metastasis (LM) models in a dose-dependent manner (starting from 7.5mg/kg qd), as well as significantly prolonged animal survival in these two models.查看更多
有个活性分子后，如何确定最优的盐和晶型?盐： Handbook of pharmaceutical salts, by P. Heinrich (EDT) and Wermuth Stahl 晶型：Polymorphism: in the pharmaceutical industry, by Rolf Hilfiker 这两本是最经典的，够学三五年的。 请问这俩书哪里有呢查看更多
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