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KW-2449  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥50 mg/mL）
产品描述：基本信息 产品编号：K10085 产品名称：KW-2449 CAS: 1000669-72-6   储存条件 粉末 -20℃ 四年     分子式： C20H20N4O 溶于液体 -80℃ 六个月 分子量 332.40 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 67mg/mL (201.56mM) Ethanol 67mg/mL (201.56mM) Water Insoluble 体内（现配现用） 0.5%methylcellulose 30mg/mL ＜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 3.0084mL 15.0421mL 30.0842mL 5mM 0.6017mL 3.0084mL 6.0168mL 10mM 0.3008mL 1.5042mL 3.0084mL 50mM 0.0602mL 0.3008mL 0.6017mL   生物活性 产品描述 一种多靶点激酶抑制剂，对FLT3，ABL，ABLT315I和 Aurora kinase 的 IC50 值分别为6.6，14，4 和 48 nM。 靶点/IC50 FLT3 (D835Y)(Cell-free assay) Abl (T315I)(Cell-free assay) FLT3(Cell-free assay) Abl(Cell-free assay) FGFR1(Cell-free assay) 1nM 4nM 6.6nM 14nM 36nM 体外研究 KW-2449 shows growth inhibitory activities against FLT3/ITD-, FLT3/D835Y-, and wt-FLT3/FL-expressing 32D cells, MOLM-13 and MV4;11 with GI50 values of 0.024,0.046, 0.014, 0.024, and 0.011μM, respectively. KW-2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dosedependent manner.KW-2449 increases the percentage of cells in the G1 phase of the cell cycle and reciprocally reduced the percentage of cells in the S phase, resulting in the increase of apoptotic cell population. 体内研究 Oral administration of KW-2449 shows dose-dependent and significant tumor growth inhibition in FLT3-mutated xenograft model with minimum bone marrow suppression. In FLT3 wild-type human leukemia, it induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis. In imatinib-resistant leukemia, KW-2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases. Furthermore, the antiproliferative activity of KW-2449 is confirmed in primary samples from AML and imatinib-resistant patients.The inhibitory activity of KW2449 is not affected by the presence of human plasma protein, such as α1-acid glycoprotein.   推荐实验方法(仅供参考) 细胞实验:   Cell viability is determined by the sodium 3′-[1-(phenylaminocarbonyl)-3, 4-tetrazolium]-bis (4-methoxy-6-nitro) benzene sulfonic acid hydrate assay after incubation with or without KW-2449 for 72 hours at 37℃. The number of viable cells is determined using the Cell Proliferation Kit II.   动物实验:   Mice: SCID mice are subcutaneously inoculated with MOLM-13 cells. Five days after inoculation, tumor volume is measured using the Antitumor test system II. The 25 mice with tumors ranging from 90 to 130 mm3 are selected and randomized using the Antitumor test system II. From the day of randomization, vehicle (0.5 wt/vol% MC400) or KW-2449 (2.5, 5.0, 10, and 20mg/kg) is orally administered to mice twice a day for 14 days. Tumor volume is measured twice a week during the treatment.
保存条件：-20℃

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