Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD0166285是 P-gp 的底物,是一种有效的 Wee1 和 Chk1 抑制剂弱抑制。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 497 | 现货 | ||
2 mg | ¥ 729 | 现货 | ||
5 mg | ¥ 1,190 | 现货 | ||
10 mg | ¥ 1,930 | 现货 | ||
25 mg | ¥ 3,270 | 现货 | ||
50 mg | ¥ 4,770 | 现货 | ||
100 mg | ¥ 6,780 | 现货 | ||
500 mg | ¥ 13,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,380 | 现货 |
产品描述 | PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator. |
靶点活性 | Chk1:3.4 μM, Myt1:72 nM, Wee1:24 nM |
体外活性 | PD0166285 is identified to inhibit Wee1 activity at nanomolar concentrations. The inhibitor abrogates G2/M checkpoint inducing early cell division. At the cellular level, 0.5 μM PD0166285 dramatically inhibits irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in seven of seven cancer cell lines tested. This G2 checkpoint abrogation by PD0166285 is demonstrated to kill cancer cells. PD0166285 does not inhibit Cdc2/cyclin B but inhibits Chk1 kinase at a much higher concentration (3433 nM). the treatment of cells with the inhibitor is related to microtubule stabilization and decrease in cyclin D transcription. Thus, PD0166285 may be a potentially useful anti-cancer therapy[1][2]. |
体内活性 | PD0166285 at 0.5 μM concentration can inhibit Cdc2Y15 /T14 phosphorylation in all cell lines tested, regardless of their p53 status[1] and pharmacological targeting of WEE1 by PD0166285 sensitizes U251-FM GBM tumors to IR in vivo[3]. |
激酶实验 | Wee1 Mass Screening: Wee1 mass screening is performed using Amersham's p34cdc2 kinase SPA kit with some modifications. Briefly, 45–60 nM full-length Wee1 kinase is incubated with 25 μM compounds, 20 μM ATP, and 122–441 nM Cdc2/cyclin B in a final volume of 50 μl of enzyme dilution buffer [50 mM Tris (pH 8.0), 10 mM NaCl, 10 mM MgCl2, 1 mM DTT, and 0.1 mM Na3VO4]. After 30 min incubation at 30°C, 30 μl of [33P]ATP containing kinase buffer [67 mM Tris (pH 8.0), 40 mM NaCl, 13 mM MgCl2, 1 mM DTT, and 0.13 mM Na3VO4] containing 1 μM biotinylated peptide, and 0.25 μCi of [γ-33P]ATP is added to the reaction and incubated for another 30 min at 30°C. The reaction is stopped by adding 200 μl of stop buffer [50 μM ATP, 5 mM EDTA, 0.1% Triton X-100, and 1.25 mg/ml SPA beads in PBS]. After centrifugation at 2400 rpm for 15 min, the plate is counted with Wallac's Microbeta counter. |
细胞实验 | B16 cells (1 × 105 cells in 100 mm-dishes) are maintained in medium overnight. In addition, the cells are treated with (0, 0.5, 1.0, or 2.0 μM) PD0166285 (including DMSO vehicle) for indicated times. The cells are washed twice with phosphate-buffered saline (PBS). Next, the cells are trypsinized, so the cell numbers in each dish are determined by using a computed cell-counter (Sysmex CDA-500) according to manufacturer's recommendation. (Only for Reference) |
动物实验 | E98 tumor fragments (8 mm3) were grafted subcutaneously in the flank of Balb/C nude mice (n = 10). For the experiments with the orthotopic tumors, U251 mg and E98 cells were transduced to express Fluc and mCherry, to generate U251-FM and E98-FM cells. One million cells were injected intracranially. Starting at 12 days after tumor inoculation, mice received the WEE1 inhibitor PD0166285 via intraperitoneal injections (500 μl of a 20 μM solution diluted in NaCl) or vehicle for 5 consecutive days. On days 10–15, mice were irradiated with a single dose of irradiation. |
别名 | PD-166285 |
分子量 | 512.43 |
分子式 | C26H27Cl2N5O2 |
CAS No. | 185039-89-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 93 mg/mL (181.5 mM)
DMSO: 93 mg/mL (181.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.9515 mL | 9.7574 mL | 19.5149 mL | 48.7872 mL |
5 mM | 0.3903 mL | 1.9515 mL | 3.903 mL | 9.7574 mL | |
10 mM | 0.1951 mL | 0.9757 mL | 1.9515 mL | 4.8787 mL | |
20 mM | 0.0976 mL | 0.4879 mL | 0.9757 mL | 2.4394 mL | |
50 mM | 0.039 mL | 0.1951 mL | 0.3903 mL | 0.9757 mL | |
100 mM | 0.0195 mL | 0.0976 mL | 0.1951 mL | 0.4879 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。
PD0166285 185039-89-8 Apoptosis Cell Cycle/Checkpoint Wee1 Chk PD 166285 Inhibitor inhibit PD-166285 PD166285 PD-0166285 PD 0166285 inhibitor