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ISCK03  ≥98%(HPLC)

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包装规格：5mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO( ≥20 mg/mL )
产品描述：基本信息 产品编号：I10017 产品名称：ISCK03 CAS: 945526-43-2   储存条件 粉末 -20℃ 四年     分子式： C19H21N3O2S 溶于液体 -80℃ 六个月 分子量 355.45 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 71mg/mL (199.74mM) Ethanol 3mg/mL (8.44mM) 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 2.8133mL 14.0667mL 28.1334mL 5mM 0.5627mL 2.8133mL 5.6267mL 10mM 0.2813mL 1.4067mL 2.8133mL 50mM 0.0563mL 0.2813mL 0.5627mL   生物活性 产品描述 一种c-kit活性抑制剂。 靶点/IC50 SCF c-Kit   体外研究 Pretreatment of 501mel cells with ISCK03 inhibits SCF-induced c-kit phosphorylation dose dependently. ISCK03 also inhibits p44/42 ERK mitogen-activated protein kinase (MAPK) phosphorylation, which is known to be involved in SCF/c-kit downstream signaling. However ISCK03 does not inhibit hepatocyte growth factor (HGF)-induced phosphorylation of p44/42 ERK proteins. ISCK03, a tyrosine kinase inhibitor specific to KIT, prevents survival of CCDC26-KD cells under low-serum conditions. All treated cells exhibits sensitivity to ISCK03 in a dose-dependent manner. After ISCK03 treatment, the survival of KD cells is suppressed to the same level as that of non-KD cells. Conversely, ISCK03 treatment has limited effects on the growth of control K562 and KD clone 3–4 cells under high-serum concentration conditions.   体内研究 Oral administration of ISCK03 induces the dose-dependent depigmentation of newly regrown hair, and this is reversed with cessation of ISCK03 treatment. The topical application of ISCK03 promotes the depigmentation of UV-induced hyperpigmented spots. Fontana-Masson staining analysis shows epidermal melanin is diminished in spots treated with ISCK03.   推荐实验方法(仅供参考) 激酶实验： ATP is dispensed into 384-well plates, chemical compounds (ISCK03: 2.5, 5, 10, 100μM) are added by replicative plate, and recombinant human c-kit protein is added for the kinase reaction.Following a 45-min incubation at 37℃, the development reaction is carried out for 40min at room temperature. After the reaction is stopped, the coumrain and fluorescein fluorescence-emission signals are detected.   细胞实验:   To determine any cytotoxic effects of ISCK03 on 501mel cells, MTT assays are performed with various doses of ISCK03 (1, 5,10μM). 501mel cells are cultured with SCF alone (50ng/mL) or SCF with ISCK03 for 48h.   动物实验:   Mice: To induce the hair cycle, depilation of skin on the back of the female C57BL/6 mice is performed. Briefly, the hair is removed from anesthetized mice. The rat antimouse c-kit-neutralizing monoclonal antibody ACK2 is administered intraperitoneally (50mg) every day.ISCK03 is administered orally once a day. On days 21–28, animals are sacrificed or analyzed for repigmentation of the newly regrown hair shaft. Skin is harvested and fixed in paraffin or frozen for immunohistochemical analyses.
保存条件：-20℃

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