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D-I03  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥ 100 mg/mL）
产品描述：基本信息 产品编号：D10803 产品名称：D-I03 CAS: 688342-78-1   储存条件 粉末 -20℃ 四年     分子式： C13H20N2O2 溶于液体 -80℃ 两年 分子量 428.64 -20℃ 一个月 化学名：  N-[2-(diethylamino)ethyl]-N'-[2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl]thiourea   Solubility (25°C)   体外 DMSO 86mg/mL (200.63mM) Ethanol 10mg/mL (23.32mM) 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。     制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3330mL 11.6648mL 23.3296mL 5mM 0.4666mL 2.3330mL 4.6659mL 10mM 0.2333mL 1.1665mL 2.3330mL 50mM 0.0467mL 0.2333mL 0.4666mL     生物活性 产品描述 一种选择性 RAD52 抑制剂，Kd 为 25.8μM。D-I03 抑制 RAD52 依赖性单链退火 (SSA) 和 D 环形成，IC50 分别为 5μM 和 8μM。 靶点/IC50 RAD52 (Cell-free assay) 25.8μM(Ki)   体外研究 D-I03 (0-10μM; on days 1 and 3; Capan-1 and UWB1.289 cells) treatment preferentially suppressed the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner. D-I03 inhibits RAD52 foci formation induced by cisplatin in BCR-ABL1-positive BRCA1-deficient 32Dcl3murine hematopoietic cell line that expresses GFP-RAD52. In the presence of D-I03 (2.5μM), the fraction of cells with RAD52 foci is decreased, from 38.7% to 171%; at the same time, the fraction of Cisplatin-treated cells without foci is increased from 48.4% to 71.9%. D-I03 does not effect on RAD51 foci induced by Cisplatin. Also, D-I03 alone induce neither RAD51 foci nor RAD52 foci (in BRCA1- deficient cells) indicating low genotoxicity of D-I03. Cell Proliferation Assay Cell Line: Capan-1 (BRCA2− ) and UWB1.289 (BRCA1+ ) cells Concentration: 0μM, 2.5μM, 5μM, or 10μM Incubation Time: On days 1 and 3 Result: Preferentially suppressed the growth of Capan-1 and UWB1.289 cells.   体内研究 D-I03 (50 mg/kg/day; intraperitoneal injection; daily; for 7 days; nu/nu mice) treatment reduces BRCA1-deficient MDA-MB436 tumor growth. Talazoparib puls D-I03 does not affect the growth of BRCA1-proficient tumors and does not exert any significant toxicity against normal tissues and organs. Pharmacokinetic and toxicity studies indicates that maximal tolerated dose of D-I03 is ≥50mg/kg, and t1/2 is 23.4 hours, resulting in >1μM maximal concentration in peripheral blood. Animal Model: Nu/nu mice injected with BRCA1-deficient MDA-MB-436 cells Dosage: 50mg/kg/day Administration: Intraperitoneal injection; daily; for 7 days Result: Reduced BRCA1-deficient MDA-MB-436 tumor growth.
保存条件：-20℃

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