Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PP121是一种多靶点激酶抑制剂,抑制 PDGFR、Hck、mTOR、VEGFR2、Src、Abl、DNK-PK 的 IC50值分别为2、8、10、12、14、18、60 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 197 | 待询 | ||
5 mg | ¥ 431 | 待询 | ||
10 mg | ¥ 693 | 待询 | ||
25 mg | ¥ 1,355 | 待询 | ||
50 mg | ¥ 2,488 | 待询 | ||
100 mg | ¥ 3,333 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 498 | 现货 |
产品描述 | PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM). |
靶点活性 | mTOR:10 nM, Hck:8 nM, PDGFR:2 nM, Abl:18 nM, VEGFR2/KDR:12 nM, Src:14 nM |
体内活性 | 作用于胶质瘤细胞系(U87和LN229)时,PP-121(0.04-10 μM)可剂量依赖性地有效抑制Akt、p70S6K 和S6磷酸化。PP-121(0.04-10 μM)通过直接抑制PI3Ks 和 mTOR,而有效抑制一系列肿瘤细胞增殖。作用于LN220,U87和Seg1细胞时,PP-121可诱导细胞在G0/G1期停滞。作用于转化v-Src(Thr338)的NIH3T3 细胞,PP-121(0.08-20 μM)抑制v-Src诱导的酪氨酸磷酸化。作用于转化v-Src(Thr338)的NIH3T3细胞时,PP-121(2.5 μM)使肌动蛋白纤维的染色恢复。作用于表达C634W致癌基因 Ret突变35的TT甲状腺癌细胞时,PP-121(40 nM)抑制Ret自磷酸化。PP-121抑制 TT 甲状腺癌细胞增殖(IC50:50 nM)。作用于人脐静脉内皮细胞时,PP-121抑制VEGF刺激的细胞增殖(IC50:41 nM)。 |
激酶实验 | Kinase assays: Purified kinase domains are incubated with PP-121 at 2- or 4-fold dilutions over a concentration range of 1 nM-50 μM or with vehicle (0.1% DMSO) in the presence of 10 μM ATP, 2.5 μCi of γ-32P-ATP and substrate. Reactions are terminated by spotting onto nitrocellulose or phosphocellulose membranes, depending on the substrate; this membrane is then washed 5–6 times to remove unbound radioactivity and dried. Transferred radioactivity is quantitated by phosphorimaging and IC50 values are calculated by fitting the data to a sigmoidal doseresponse using Prism software. |
细胞实验 | For western blot analysis, cells are grown in 12-well plates and treated with PP-121 at the indicated concentrations or vehicle (0.1% DMSO). Treated cells are lysed, lysates are resolved by SDS-PAGE, transferred to nitrocellulose and blotted. For cell proliferation assays,cells are grown in 96-well plates are treated with PP-121 at 4-fold dilutions (10 μM - 0.040 μM) or vehicle (0.1% DMSO). After 72 hours cells are exposed to Resazurin sodium salt (22 μM) and fluorescence is quantified. IC50 values are calculated using Prism software. For proliferation assays involving single cell counting, non-adherent cells are plated at low density (3–5% confluence) and treated with PP-121 (2.5 μM) or vehicle (0.1% DMSO). Cells are diluted into trypan blue daily and viable cells counted using a hemocytometer. For apoptosis and cell cycle analysis, cells are treated with the indicated concentration of PP-121 or vehicle (0.1% DMSO) for 24–72 hours. Cells are either stained live with AnnexinV-FITC or fixed with ethanol and stained with propidium iodide. Cell populations are separated using a FacsCalibur flow cytometer; data is collected using CellQuest Pro software and analyzed with either ModFit or FlowJo Software.(Only for Reference) |
分子量 | 319.36 |
分子式 | C17H17N7 |
CAS No. | 1092788-83-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 2 mg/mL (6.26 mM)
DMSO: 60 mg/mL (187.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.1313 mL | 15.6563 mL | 31.3126 mL | 78.2816 mL |
5 mM | 0.6263 mL | 3.1313 mL | 6.2625 mL | 15.6563 mL | |
DMSO | 10 mM | 0.3131 mL | 1.5656 mL | 3.1313 mL | 7.8282 mL |
20 mM | 0.1566 mL | 0.7828 mL | 1.5656 mL | 3.9141 mL | |
50 mM | 0.0626 mL | 0.3131 mL | 0.6263 mL | 1.5656 mL | |
100 mM | 0.0313 mL | 0.1566 mL | 0.3131 mL | 0.7828 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。
PP121 1092788-83-4 Angiogenesis Apoptosis Cytoskeletal Signaling PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors VEGFR Bcr-Abl PDGFR Src mTOR Hck Platelet-derived growth factor receptor PP 121 PP-121 inhibit Inhibitor Mammalian target of Rapamycin Vascular endothelial growth factor receptor inhibitor