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PD180970  ≥98%

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产品描述：基本信息 产品编号：P60048 产品名称：PD180970 CAS: 287204-45-9   储存条件 粉末 -20℃ 四年 分子式： C21H15Cl2FN4O 溶于液体     分子量 429.27     化学名：      Solubility (25°C)   体外 DMSO 92mg/mL (200.04mM) Ethanol Insoluble Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 生物活性 产品描述 一种高效且具有 ATP 竞争性的 p210Bcr-Abl 激酶抑制剂，可抑制 p210Bcr-Abl 的自磷酸化，IC50 为 5nM。PD180970 还抑制 Src 和 KIT 激酶，IC50 分别为 0.8nM 和 50nM。PD180970 可诱导 K562 白血病细胞凋亡 (apoptosis)，可用于慢性粒细胞白血病的研究。 靶点/IC50 Bcr-Abl 5nM (IC50, p210Bcr-Abl kinase) Src 0.8nM (IC50) KIT 50nM (IC50)   体外研究 PD180970 (0.5μM; 24-96 hours) treatment causes cell death K562 cells. PD180970 (0.5μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI doublepositive cells. PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170nM, 80nM, and 80nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210Bcr-Abl (IC50 of 5nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 of 2.2nM). The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNAbinding activity with an IC50 of 5nM.Cell Viability Assay Cell Line: K562 cells Concentration: 0.5μM Incubation Time: 24 hours, 48 hours, 72 hours, 96 hours Result: Resulted in cell death. Apoptosis Analysis Cell Line: K562 cells Concentration: 0.5μM Incubation Time: 24 hours, 48 hours Result: Increased annexin V-positive/PI-negative cells.   体内研究 PD180970 (5mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson's disease (PD). Animal Model: Male C57BL/6J mice (3-4 months old) injected with MPTP Dosage: 5mg/kg Administration: Intraperitonial injection; daily; for 7 days Result: Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia.
保存条件：-20℃

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