store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD173955是一种Src 激酶家族选择性抑制剂,对Src、Yes 和Abl 激酶IC50值约为22nM, 对 FGFRα 的效力较低,对InsR 和PKC 无活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 551 | 现货 | ||
2 mg | ¥ 803 | 现货 | ||
5 mg | ¥ 1,180 | 现货 | ||
10 mg | ¥ 1,890 | 现货 | ||
25 mg | ¥ 3,190 | 现货 | ||
50 mg | ¥ 4,580 | 现货 | ||
100 mg | ¥ 6,450 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,320 | 现货 |
产品描述 | PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC. |
靶点活性 | Src:22 nM |
体内活性 | PD173955作为Src抑制剂,在各类型细胞早期有丝分裂期间有效抑制有丝分裂进程,并诱导不同程度的细胞凋亡。PD173955有效抑制Bcr-Abl依赖性细胞生长,在Bcr-Abl阳性细胞系中IC50为2-35 nM,比Bcr-Abl阴性细胞系灵敏度高约100到200倍。通过抑制试剂盒配体依赖性c-kit自身磷酸化,PD173955也会抑制M07e细胞的试剂盒配体依赖性增殖,IC50为40 nM。 |
激酶实验 | In Vitro Bcr-Abl Kinase Assays: Bcr-Abl complexed to SHIP2 is immunoprecipitated from cell lysates of K562 cells maintained in log-phase culture conditions. Complexes are collected on protein A-Sepharose, and complexes are washed three times in lysis buffer and then washed twice in abl kinase buffer [50 mM Tris (pH 8.0), 10 mM MgCl2, 1 mM DTT, 2 mM p-nitrophenylphosphate, and 2 μM ATP; New England Biolabs Buffer and protocol]. Kinase assays are performed with 10 μM [γ-32P]ATP/sample for 15–60 min at 30°C in the presence or absence of the indicated concentrations of drug. The reaction is stopped by the addition of SDS-PAGE sample buffer and heated at 100°C for 10 min. Proteins are separated on 7.5% SDS-polyacrylamide gels, gels are dried under vacuum, and phosphorylation is visualized by autoradiography on X-ray film. |
细胞实验 | Cell growth is determined by two methods. For the [3H]thymidine assay, cells (104 cells/well) are cultured in 96-well, round-bottomed plates with diluted DMSO (control) or with varying concentrations of a specific compound that is resuspended in DMSO for 48 h at 37°C. [3H]Thymidine is added at a concentration of 1 μCi/well, and cells are incubated for an additional 18 h. Cells were harvested with the Unifilter system, scintillation fluid (25 μl/well) is added to each well, and [3H]thymidine incorporation is determined on a Packard Scintillation Counter. Data points for all assays are obtained in triplicate, and background incorporation from cell-free wells is determined and subtracted from all data points. For cell viability, control and drug-treated harvested cells are counted on a hemocytometer using the trypan blue dye exclusion method.(Only for Reference) |
别名 | PD-173955, PD 173955 |
分子量 | 443.35 |
分子式 | C21H16Cl2N4OS |
CAS No. | 260415-63-2 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 12 mg/mL (27.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2556 mL | 11.2778 mL | 22.5555 mL | 56.3889 mL |
5 mM | 0.4511 mL | 2.2556 mL | 4.5111 mL | 11.2778 mL | |
10 mM | 0.2256 mL | 1.1278 mL | 2.2556 mL | 5.6389 mL | |
20 mM | 0.1128 mL | 0.5639 mL | 1.1278 mL | 2.8194 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。
PD173955 260415-63-2 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl Src inhibit Inhibitor PD-173955 PD 173955 inhibitor