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JK184  ≥98%

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO（≥50mg/mL）
产品描述：基本信息 产品编号： J50001  产品名称： JK184 CAS: 315703-52-7   储存条件 粉末 -20℃ 四年     分子式： C19H18N4Os 溶于液体 -80℃ 两年 分子量 350.44 -20℃ 1个月 化学名：  Jagged-1 (188-204) (TFA)  N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine Solubility (25°C)：   体外:   DMSO 70 mg/mL (199.74mM) Ethanol 14 mg/mL (39.94mM) Water Insoluble 体内(现配现用): 1.请依序添加每种溶剂： 10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5 mg/mL (7.13mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (7.13mM，饱和度未知) 的澄清溶液。 以 1mL 工作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加入50μL Tween-80，混合均匀；然后继续加入 450μL生理盐水定容至 1mL。 2.请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (7.13mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (7.13mM，饱和度未知) 的澄清溶液。 以 1mL 工作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3.请依序添加每种溶剂： 10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (7.13mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (7.13mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1mL 工作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL玉米油中，混合均匀。 ＜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 2.8536mL 14.2678mL 28.5356mL 5mM 0.5707mL 2.8536mL 5.7071mL 10mM 0.2854mL 1.4268mL 2.8536mL 50mM 0.0571mL 0.2854mL 0.5707mL   生物活性 产品描述 一种有效的 Hedgehog (Hh) 抑制剂，在哺乳动物细胞中，IC50 为 30nM 靶点 IC50: 30nM (Hedgehog) 体外研究 JK184 is designed to antagonize Hh signaling by inhibiting glioma (Gli)-dependent transcriptional activity in a dose dependent manner. JK184 significantly inhibitts proliferation of HUVECs with IC50 of 6.3μg/mL after three days incubation. To evaluate anti-tumor effect of JK184, MTT assay is conducted in Panc-1 and BxPC-3 cells after administration with indicated concentrations of compounds, half maximal inhibitory concentration (IC50) of JK184 (23.7ng/mL in anc-1 and 34.3ng/mL in BxPC-3). Claudin-low cell lines are more sensitive to JK184 treatment than are MCF10a, MTSV1-7, or HMLE-shGFP and HMLE-pBP cells, and JK184 induced a dose-dependent decrease in glioma-associated oncogene homolog 1 (GLI1) transcript and protein levels in these cells. Treatment with the IC50 dose of JK184 enhances the proportion of HMLE-shEcad cells that stained with Annexin-V, but are negative for propidium iodide (PI) (P<0.0001, t test). 体内研究 JK184 (5 mg/kg, injected intravenously) exhibits good anti-proliferative activity in subcutaneous Panc-1 and BxPC-3 tumor models, and is a good candidate as antitumor drug targeted Hh signaling. However, JK184 has a poor pharmacokinetic profile and bioavailability .   推荐实验方法(仅供参考) Cell Assay The Shh-LIGHT2 cells are seeded in 96-well plates and grown to confluency. The Shh-LIGHT2 cells are treated with various concentrations of JK184 micelles or free JK184 or micelles in DMEM containing 0.5% CS, 0.1 mg/mL streptomycin, 100 U/mL penicillin, 5% Shh-N conditioned medium obtained from Shh-N-producing HEK293 cells. The treated cells are cultured further for 60 h, and firefly and Renilla luciferase activities are measured using a dual luciferase kit. Proliferation assay or apoptosis evaluation of HUVECs is measured using MTT method or FCM analysis, respectively. HUVECs are treated with a series concentration of free JK184, JK184 micelles, or blank MPEG-PCL micelles for 48 h, respectively. The mean percentage of cell inhibition or apoptosis is calculated   Animal Administration MiceFive-week-old female athymic (nu/nu) mice are used. BxPC-3 and Panc-1 tumors are established by s.c. injection of 1×107 cells. Mice bearing tumors around 100 mm3 are selected and randomized into treatment groups (5 mice per group). Mice are injected intravenously every day for 30 days with 100 μL of NS (control), blank micelles, free JK184 (5 mg/kg body weight), or JK184 micelles (5 mg/kg body weight), respectively. Tumor length and width are determined every 3 days and tumor volume (TV) is calculated using the following formula: TV=0.5×length×width2. At the end of experiment, mice are sacrificed. Solid tumors are removed and processed for immunohistochemical analysis and terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assay.
保存条件：-20℃

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