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Desmethyl Erlotinib hydrochloride

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产品编号 T6619Cas号 183320-51-6
别名 去甲厄洛替尼, OSI-420, OSI420, OSI 420, DesMethyl Erlotinib (CP-473420) HCl, Desmethyl Erlotinib, CP-473420

Desmethyl Erlotinib hydrochloride (OSI 420) 是 Erlotinib 的活性代谢物。Erlotinib 是 EGFR 酪氨酸激酶抑制剂。

Desmethyl Erlotinib hydrochloride

Desmethyl Erlotinib hydrochloride

Rating icon 很棒
纯度: 99.03%
产品编号 T6619 别名 去甲厄洛替尼, OSI-420, OSI420, OSI 420, DesMethyl Erlotinib (CP-473420) HCl, Desmethyl Erlotinib, CP-473420Cas号 183320-51-6

Desmethyl Erlotinib hydrochloride (OSI 420) 是 Erlotinib 的活性代谢物。Erlotinib 是 EGFR 酪氨酸激酶抑制剂。

规格价格库存数量
1 mg¥ 453现货
2 mg¥ 641现货
5 mg¥ 935现货
10 mg¥ 1,730现货
25 mg¥ 2,950现货
50 mg¥ 4,360现货
100 mg¥ 6,220现货
500 mg¥ 12,700现货
1 mL x 10 mM (in DMSO)¥ 995现货
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纯度:99.03%
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产品介绍

生物活性
产品描述
Desmethyl Erlotinib hydrochloride (OSI 420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for human EGFR and EGFR autophosphorylation in tumor cells.
靶点活性
EGFR:2 nM
体外活性
OSI-420 is the major metabolite of Erlotinib in human plasma. Erlotinib disappearance from plasma after a short IV infusion is biexponential with a mean terminal half-life of 5.2 h and a mean clearance of 128 ml/min per m(2). OSI-420 exposure (AUC) in plasma is 30% (range 12-59%) of erlotinib, and OSI-420 clearance is more than 5-fold higher than erlotinib. Erlotinib and OSI-420 are equipotent, and the combined concentrations of erlotinib + OSI-420 achieved in the CSF exceeded the IC50 (7.9 ng/ml or 20 nM) for the EGFR tyrosine kinase inhibition in intact tumor cells. [1] Erlotinib potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20 nM), DiFi human colon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib (1 μM) induces apoptosis in DiFi human colon cancer cells. [2] Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. [3] Erlotinib(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. [4] The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. [5] Combination with Erlotinib could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. [6]
体内活性
At doses of 100 mg/kg, Erlotinib completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. [1] Erlotinib reduces the growth of xenografted human AML cells. [4]
激酶实验
Kinase Assays: 96-well plates are coated by incubation overnight at 37 °C with 100 μL per well of 0.25 mg/mL PGT in PBS. Excess PGT is removed by aspiration, and the plate is washed 3 times with washing buffer (0.1% Tween 20 in PBS). The kinase reaction is performed in 50 μL of 50 mM HEPES (pH 7.3), containing 125 mM sodium chloride, 24 mM magnesium chloride, 0.1 mM sodium orthovanadate, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of EGFR, affinity purified from A431 cell membranes. Erlotinib HCl in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8 minutes at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with washing buffer. Phosphorylated PGT is measured by 25 minutes of incubation with 50 μL per well HRP-conjugated PY54 antiphosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). Antibody is removed by aspiration, and the plate is washed 4 times with washing buffer. The colonmetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50μL per well, and stopped by the addition of 0.09 M sulfuric acid, 50 μL per well. Phosphotyrosine is estimated by measurement of absorbance at 450 nm. The signal for controls is typically 0.6-1.2 absorbance units, with essentially no back ground in wells without AlP, EGFR, or PGT and is proportional to the time of incubation for 10 minutes.
细胞实验
Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Cell viability is assayed by cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Growth inhibition is expressed as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to drug(s) compared with untreated control cells and is calculated by the CalcuSyn software. (Only for Reference)
别名去甲厄洛替尼, OSI-420, OSI420, OSI 420, DesMethyl Erlotinib (CP-473420) HCl, Desmethyl Erlotinib, CP-473420
化学信息
分子量415.87
分子式C21H21N3O4·HCl
CAS No.183320-51-6
SmilesCl.COCCOc1cc2ncnc(Nc3cccc(c3)C#C)c2cc1OCCO
密度no data available
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 77 mg/mL (185.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
1mg5mg10mg50mg
1 mM2.4046 mL12.0230 mL24.0460 mL120.2299 mL
5 mM0.4809 mL2.4046 mL4.8092 mL24.0460 mL
10 mM0.2405 mL1.2023 mL2.4046 mL12.0230 mL
20 mM0.1202 mL0.6011 mL1.2023 mL6.0115 mL
50 mM0.0481 mL0.2405 mL0.4809 mL2.4046 mL
100 mM0.0240 mL0.1202 mL0.2405 mL1.2023 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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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
%
%Tween 80
%ddH2O

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