Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD168393 是一种细胞渗透性的选择性 EGFR 酪氨酸激酶和 ErbB2的抑制剂。它不可逆转地失活 EGF 受体,IC50值为 0.7 nM,但对胰岛素受体、PDGFR、FGFR 和 PKC 无作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 448 | 现货 | ||
5 mg | ¥ 637 | 现货 | ||
10 mg | ¥ 1,098 | 现货 | ||
25 mg | ¥ 2,179 | 现货 | ||
50 mg | ¥ 3,859 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 519 | 现货 |
产品描述 | PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin. |
靶点活性 | EGFR:0.70 nM |
体外活性 | PD 168393 is docked into the ATP binding pocket of EGFR TK. PD168393 completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continous suppression even after 8 hr in compound-free medium. PD168393 inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. PD168393 is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. PD168393 inhibits EGF-mediated tyrosine phosphorylation in HS-27 human fibroblasts with IC50 of 1-6 nM but has little effect on FGF- or PDGF-mediated tyrosine phosphorylation. [1] PD168393 shows rapid and potent inhibition of Her2-induced tyrosine phosphorylation with IC50 of ~100 nM in 3T3-Her2 cells. D168393 also inhibits phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin in 3T3-Her2 cells, except for Fyb. [2] |
体内活性 | PD 168393 produces tumor growth inhibition of 115% in A431 human epidermoid carcinoma xenograft in nude mice, with 50% reduced phosphotyrosine content of EGFR. PD 168393 also shows a low plasma concentration. [1] |
激酶实验 | The effects of VU0364770 on rat mGlu1 and mGlu5 are assessed by using calcium mobilization and measuring the glutamate concentration-response relationship in the presence and absence of 10 μM VU0364770. Using a double-addition protocol, VU0364770 is added to the cells, followed 2.5 min later by a full concentration-response of glutamate. Shifts of the concentration-response relationship are used to assess potential potentiator (left shift of more than 2-fold) or antagonist (right shift of more than 2-fold or depression of the maximum response by at least 75%) activity of VU0364770. Compounds are further assessed for mGlu5 antagonist activity by performing a full concentration-response curve, starting at 30 μM and serially diluted it by using 1:3 dilutions, in the presence of an EC80 concentration of glutamate[1]. |
分子量 | 369.22 |
分子式 | C17H13BrN4O |
CAS No. | 194423-15-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 68 mg/mL (184.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7084 mL | 13.5421 mL | 27.0841 mL | 67.7103 mL |
5 mM | 0.5417 mL | 2.7084 mL | 5.4168 mL | 13.5421 mL | |
10 mM | 0.2708 mL | 1.3542 mL | 2.7084 mL | 6.771 mL | |
20 mM | 0.1354 mL | 0.6771 mL | 1.3542 mL | 3.3855 mL | |
50 mM | 0.0542 mL | 0.2708 mL | 0.5417 mL | 1.3542 mL | |
100 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL | 0.6771 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。
PD168393 194423-15-9 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic Cytoskeletal Signaling JAK/STAT signaling Tyrosine Kinase/Adaptors FGFR EGFR PDGFR PKC IGF-1R ErbB-1 PD 168393 HER1 Epidermal growth factor receptor tumor epidermoid carcinoma PD-168393 Inhibitor inhibit inhibitor