Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WHI-P154 (Jak3 inhibitor ii) 是一种 EGFR 抑制剂,也抑制 JAK3的活性,IC50值分别为 4 nM 和 1.8 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 197 | 现货 | ||
5 mg | ¥ 415 | 现货 | ||
10 mg | ¥ 685 | 现货 | ||
25 mg | ¥ 1,450 | 现货 | ||
50 mg | ¥ 2,550 | 现货 | ||
100 mg | ¥ 3,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 460 | 现货 |
产品描述 | WHI-P154 (Jak3 inhibitor ii) is a potent JAK3 inhibitor. |
靶点活性 | EGFR:4 nM, VEGFR:100 nM, JAK3:1.8 μM, Src:100 nM |
体外活性 | 体内使用EGF-P154导致严重联合免疫缺陷小鼠成胶质细胞瘤异种移植模型中的肿瘤生长延迟并且改善无瘤存活.然而无瘤小鼠生存期都没有超过33天 (无瘤生存期中值为19天),并且所有对照小鼠的肿瘤在58天内迅速达到平均尺寸> 500 mM3,用1 mg/kg/天 EGF-P154连续治疗10天的小鼠中有40%活下来并且58天以上没有检测到肿瘤,无瘤生存期中值为40天.剩下的60%小鼠中肿瘤体积从未超过50 mm3. |
体内活性 | WHI-P154的体外抗胶质母细胞瘤活性扩增> 200倍,并通过结合重组人源表皮生长因子而具有选择性。WHI-P154在体外抑制巨噬细胞中STAT1激活,iNOS表达和NO产生。研究证明,WHI-P154还可以抑制其它常见激酶,包括EGFR,Src,Abl,VEGFR,MAPK和PI3-K,并诱导人成胶质细胞瘤细胞系中的细胞凋亡。WHI-P154在ECM中抑制胶质母细胞瘤细胞粘附和迁移。 WHI-P154 对人恶性胶质瘤细胞系U373和U87具有明显的细胞毒性,在微摩尔浓度下引起凋亡性细胞死亡。 |
激酶实验 | Kinase assays: WHI-P154 is tested in kinase assays. The panel of kinases is selected to broadly cover the kinome, providing a good approximation of specificity. For all kinases, recombinant rat (IKKβ) or human (all others), full-length or GST-kinase domain fusion proteins, are used. WHI-P154 is inactive (concentration that inhibits response by 50% [IC50] > 30 μM) for the following kinases: AKT, AuroraA, cdk2, cdk6, CHK1, FGFR1, GSK3b, IKKb, IKKi, INSR, MAPK1, MAPKAP-K2, MASK, MET, PAK4, PDK1, PKCb, ROCK1, TaoK3, TrkA. |
细胞实验 | Cells are seeded into a 96-well plate at a density of 2.5×104 cells/well and incubated for 36 h at 37 ℃ before drug exposure. On the day of treatment, culture medium is carefully aspirated from the wells and replaced with fresh medium containing the quinazoline compounds WHI-P154 at concentrations ranging from 0.1 μM to 250 μM. Triplicate wells are used for each treatment. The cells are incubated with the compound for 24hours to 36hours at 37 ℃ in a humidified 5% CO2 atmosphere. To each well, 10 μL of MTT (final concentration, 0.5 mg/mL) is added, and the plate are incubated at 37 ℃ for 4 h. Than solubilized overnight at 37 ℃ in a solution containing 10% SDS in 0.01 M HCL. The absorbance of each well is measured in a microplate reader at 570 nm.(Only for Reference) |
别名 | Jak3 inhibitor ii |
分子量 | 376.2 |
分子式 | C16H14BrN3O3 |
CAS No. | 211555-04-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 37.6 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6582 mL | 13.2908 mL | 26.5816 mL | 66.454 mL |
5 mM | 0.5316 mL | 2.6582 mL | 5.3163 mL | 13.2908 mL | |
10 mM | 0.2658 mL | 1.3291 mL | 2.6582 mL | 6.6454 mL | |
20 mM | 0.1329 mL | 0.6645 mL | 1.3291 mL | 3.3227 mL | |
50 mM | 0.0532 mL | 0.2658 mL | 0.5316 mL | 1.3291 mL | |
100 mM | 0.0266 mL | 0.1329 mL | 0.2658 mL | 0.6645 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
WHI-P154 211555-04-3 Angiogenesis Apoptosis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors EGFR VEGFR JAK Src Janus kinase Jak3 inhibitor ii WHI-P-154 WHI-P 154 ErbB-1 inhibit Epidermal growth factor receptor HER1 WHIP154 Inhibitor WHI P154 inhibitor