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PD168393

PD168393

产品编号 T6932   CAS 194423-15-9

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、PDGFRFGFRPKC 无作用。

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PD168393 Chemical Structure
PD168393, CAS 194423-15-9
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
产品目录号及名称: PD168393 (T6932)
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纯度: 99.7%
纯度: 99.13%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 68 mg/mL (184.2 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Fry W, et al. Proc Natl Acad Sci U S A. 1998, 95(20), 12022-12027. 2. Bose R, et al. Proc Natl Acad Sci U S A, 2006, 103(26), 9773-9778.
5Z-7-Oxozeaenol N-Desmethyl imatinib Dovitinib lactate Avapritinib KI8751 ZM323881 hydrochloride AC710 Mesylate Ki20227

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 TGF-β/Smad靶点化合物库 抗癌活性化合物库 酪氨酸激酶分子库 半胱氨酸共价化合物库 干细胞分化化合物库 JAK-STAT 化合物库 抗前列腺癌化合物库 抗心血管疾病化合物库 成骨分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

PD168393 194423-15-9 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic Cytoskeletal Signaling JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR FGFR IGF-1R PDGFR PKC ErbB-1 PD 168393 HER1 Epidermal growth factor receptor tumor epidermoid carcinoma PD-168393 Inhibitor inhibit inhibitor

 

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