Erlotinib HCl (OSI-744)
目录号：S1023 别名： (CP358774, NSC 718781) HCl
Molecular Weight(MW): 429.90
Erlotinib HCl (OSI-744)是一种EGFR抑制剂，在无细胞试验中IC50为2 nM，对EGFR的选择性比对人c-Src或v-Abl高1000多倍。
客户使用该产品的17个实验数据：
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Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers.
Nat Genet 2012 44(8):852-60. Erlotinib HCl (OSI-744) purchased from Selleck.
J Clin Invest 2012 122, 3197-210. Erlotinib HCl (OSI-744) purchased from Selleck.
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Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone.
Cancer Res 2014 4(1):253-62. Erlotinib HCl (OSI-744) purchased from Selleck.
Immunoblots of MCF7-HER2 cells treated with DMSO (c), BEZ235 (B, 500 nM) and lapatinib (L, 500 nM) as well as with erlotinib (E, 500 nM) and the indicated combinations for 24 h.
Oncogene 2010 30, 2547-2557. Erlotinib HCl (OSI-744) purchased from Selleck.
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(B–C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 μg). The cells were then treated with Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib (20 μM), CI-1033 (8 μM), LY294002 (20 μM) and Bortezomib (20 μM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times.
Carcinogenesis 2010 31, 1948–1955. Erlotinib HCl (OSI-744) purchased from Selleck.
LNCaP-AI cells were starved in 1% stripped medium for 24 h. The cells were then treated with Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib (20 μM), CI-1033 (8 μM), LY294002 (20 μM) and Bortezomib (20 μM) for 24 h. Cell culture medium was collected from each sample and subjected to ELISA for sPLA2-IIa. The condition medium samples were diluted 10 times for ELISA. Average of duplicate samples was converted to nanogram per milliliter against standard curve. The data represent one of five repeated experiments.
Carcinogenesis 2010 31, 1948–1955. Erlotinib HCl (OSI-744) purchased from Selleck.
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Susceptibility of lung cancer cells to cytolytic activity of NK-92 cells after treatment with EGFR inhibitors. Three lung cancer cells were untreated (open circle) or treated with 10 μM erlotinib or gefitinib (black filled square or black filled triangle) for 24 hours. The lung cancer cells were cocultured with NK-92 cells at indicated effector to target ratio (E:T ratio). To determine the specificity of NKG2D-mediated cytolysis of lung cancer cells, NK-92 cells were preincubated with blocking mAb against NKG2D before the assay (gray filled square and triangle) and correspond-ing isotype mAb (open square and triangle).
J Immunother 2011 34, 372-81. Erlotinib HCl (OSI-744) purchased from Selleck.
The TMZ-induced caveolin-1 modulation is Src-dependent in Hs683 GBM cells Western blot analyses of soluble caveolin-1 expression in Hs683 glioma cells treated with TMZ (100 μM) four times per week (day 1-4) for 7 h/d, the EGFR inhibitor (10 μM) (erlotinib; day 1), the Src inhibitor AZD0530 (10 μM) (day 1), and combination of the inhibitors and TMZ (+TMZ) compared with control untreated cells (Ct). Soluble caveolin-1 expression was measured on day 5.
Transl Oncol 2011 4, 92-100. Erlotinib HCl (OSI-744) purchased from Selleck.
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miR-17-5p is down-regulated by erlotinib treatment in A549-ER cells. (A) MTT was used to assess cell viability of A549 and A549-ER cells after 72-h erlotinib treatment with different concentrations. (B) Real-time PCR quantification of indicated miRNAs. (C) Real-time PCR quantification of miR-17-5p in A549 cells treated with erlotinib at indicated concentrations for 48 h. For all, *p < 0.05, **p < 0.01, ***p < 0.001versus control group.
J Drug Target, 2016, 25(2):125-131. Erlotinib HCl (OSI-744) purchased from Selleck.
Pressure-induced myogenic tone in coronary arterioles with and without EGFR tyrosine kinase inhibitors (AG1478 and Erlotinib, 1 μM) n=6, *Pb0.05 CTR vs. EGFR inhibitor
Microvasc Res 2010 81, 135-142. Erlotinib HCl (OSI-744) purchased from Selleck.
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PAS staining and Masson's trichrome staining of kidneys in 22-week-old vehicleor erlotinib-treated AS mice.
Clin Exp Nephrol, 2017, 21(6):952-960. Erlotinib HCl (OSI-744) purchased from Selleck.
Inhibition of anchorage-independent growth of lung tumor cell lines by selected inhibitors. Each selected cell line was treated with the indicated inhibitor at 0.1 μM and 1 μM concentrations for two weeks and cell colony size formation was scored under the Nikon inverted-phase microscope.
Int J Proteomics 2011 2011, Article ID 215496. Erlotinib HCl (OSI-744) purchased from Selleck.
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Tuberc Respir Dis 2013 75(1), 9-17. Erlotinib HCl (OSI-744) purchased from Selleck.
DUSP6 is regulated by EGFR/ERK inhibition in NSCLC cell lines. Protein expression levels were assayed by immunoblot for phosphor-EGFR at indicated tyrosine sites, total-EGFR, phosphor-ERK, total-ERK, ETS1, DUSP6 and GAPDH demonstrating suppression of DUSP6 following inhibition of activated ERK (P-ERK) and ETS1 levels in the presence of appropriate drug for each of the following cell lines: (a) HCC827 cells treated with erlotinib; (b) H1975 cells treated with erlotinib or CL-387,785 (an irreversible EGFR inhibitor); H441 cells treated with (c) erlotinib or U0126 (a MEK1/2 inhibitor) and (d) erlotinib or AG1478 (specific EGFR inhibitor) (d). Cells were starved overnight with serum-free media, then treated with drug as indicated by the following abbreviations: (E) 100ng/ml EGF; (D) 0.01% DMSO control; (Er) 1 μM erlotinib, (CL) 1 μM CL-387,785, (U) 20 μM U0126 or AG1478. Whole cell lysates were obtained using 10% TCA lysis buffer and immunoblotting was performed at indicated time points.
2010 Dr. Balazs Halmos of Columbia University. Erlotinib HCl (OSI-744) purchased from Selleck.
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DUSP6 gene expression is inhibited by erlotinib using quantitative real-time PCR analysis. RNA was extracted from treated (a) HCC827 and (b) PC9 cells and relative expression level standardized against GAPDH at several time points.
2010 Dr. Balazs Halmos of Columbia University. Erlotinib HCl (OSI-744) purchased from Selleck.
Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Erlotinib for 24 hours.
2010 Dr. Zhang of Tianjin Medical University. Erlotinib HCl (OSI-744) purchased from Selleck.
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Erlotinib and picropodophyllin (PPP) act together to reduce cell proliferation. MET1 cells were cultured for 48 hours in increasing concentrations of erlotinib (A) or PPP (B) as indicated. Cell growth was then assessed using methyl thiazolyl-tetrazolium (MTT) assays. A dose-dependent decrease in the number of viable cells is seen with rising inhibitor concentrations (n = 3 at all time points). MET1 cells (C), MET4 cells (D), SCC12 cells (E), and SCC13 cells (F) were cultured for 48 hours in varying concentrations of erlotinib and PPP as indicated. Cell growth was then assayed with MTT assays. Both erlotinib and PPP demonstrated dose-dependent inhibition of cell growth, and at intermediate concentrations there seemed to be synergistic prevention of cell growth by both inhibitors. Higher concentrations of all inhibitors were also tested but are not shown as they exceeded the maximal responses of the cells to the inhibitors.
Head Neck 2013 35, 86-93. Erlotinib HCl (OSI-744) purchased from Selleck.
产品安全说明书
EGFR抑制剂选择性比较
生物活性
| 产品描述 | Erlotinib HCl (OSI-744)是一种EGFR抑制剂，在无细胞试验中IC50为2 nM，对EGFR的选择性比对人c-Src或v-Abl高1000多倍。 | |||||||||||||||||||||||
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| 靶点 |
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| 体外研究 |
Erlotinib作用于HNS人头部和颈部肿瘤细胞，有效抑制EGFR自磷酸化，HNS人头部和颈部肿瘤细胞是表达高水平EGFR的细胞系。[1] Erlotinib对SBC-5细胞增殖没有作用效果。相反, Erlotinib 显著抑制PC-9细胞增殖,这种作用存在剂量依赖性，PC-9细胞在EGFR基因第19外显子含缺失突变。Erlotinib处理也不会影响SBC-5细胞迁移。[2] Erlotinib 抑制HPAC细胞和Capan-1细胞生长， IC50 分别为1.1和3µM。10 uM Erlotinib 抑制EGFR在 Y845 (Src依赖性磷酸化) 和和Y1068(自磷酸化)位点磷酸化。[3] Erlotinib 只有作用于最敏感的细胞株时，抑制细胞外信号调节激酶, Akt, 和S6。[4] |
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| Cell Data |
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| 体内研究 | Erlotinib单独作用于H460a肿瘤模型，抑制肿瘤生长，这种作用存在剂量依赖性，与药物的循环水平相关。 |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 激酶实验：[1] |
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激酶实验: 每孔使用100 μL 溶于PBS的0.25 mg/mL PGT对96孔板包被，然后在37oC温育过夜。吸取移除过量PGT，使用冲洗 buffer (0.1% Tween-20，溶于PBS)清洗实验板3次。在 50 μL 50 mM HEPES (pH 7.3), 含125 mM NaCl, 24 mM MgCl2, 0.1 mM 原钒酸钠, 20 μM ATP, 1.6 μg/mL EGF, 以及从A431细胞膜上亲和纯化的15 ng EGFR的混合物中进行激酶反应。加入溶于 DMSO的 Erlotinib，DMSO 终浓度为2.5%。加入ATP，开始磷酸化，在室温下进行8分钟，且持续震荡。加入吸取的反应混合物，激酶反应终止，使用冲洗 buffer冲洗4次。磷酸化的PGT与50 μL每孔 HRP联合的PY54 抗磷酸抗体[在封闭液(3% BSA 和0.05% Tween-20，溶于 PBS)中稀释到0.2 μg/mL]温育25分钟后，测量磷酸化的PGT。吸取移除抗体，使用冲洗buffer冲洗实验板4次。加入 TMB 微孔过氧化物酶底物，每孔50μL，进行比色分析，然后加入0.09 M 硫酸，每孔50 μL，终止反应。在450 nm处测定吸光值而测定磷酸化。 |
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| 细胞实验：[3] |
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| 动物实验：[6] |
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溶解度 (25°C)
| 体外 | DMSO | 4 mg/mL warmed (9.3 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 15% Captisol |
16 mg/mL warmed (suspension) |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 429.90 |
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| 化学式 | C22H23N3O4.HCl |
| CAS号 | 183319-69-9 |
| 稳定性 | powder |
| in solvent | |
| 别名 | (CP358774, NSC 718781) HCl |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03720873 | Recruiting | EGFR Gene Mutation | Fujian Cancer Hospital | October 2018 | Phase 2 |
| NCT03653546 | Not yet recruiting | Non-small Cell Lung Cancer|EGFR Gene Mutation|Brain Metastases | Alpha Biopharma (Jiangsu) Co. Ltd. | August 31 2018 | Phase 2|Phase 3 |
| NCT03529084 | Withdrawn | Carcinoma Non-small Cell Lung | Novartis Pharmaceuticals|Novartis | July 23 2018 | Phase 3 |
| NCT03628521 | Recruiting | Lung Cancer|Advanced Stage | Shanghai Chest Hospital | July 20 2018 | Phase 1 |
| NCT03498521 | Recruiting | Cancer of Unknown Primary Site | Hoffmann-La Roche|Foundation Medicine Inc. | July 10 2018 | Phase 2 |
| NCT03647592 | Recruiting | Efficacy and Safety of Erlotinib Combined With Bevacizumab in EGFR Mutation Positive Advanced Non-squamous Non-small Cell Lung Cancer | Hunan Province Tumor Hospital | June 1 2018 | -- |
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如果有其他问题，请给我们留言。
常见问题及建议解决方法
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问题 1：
Whether S1023 is suitable for mouse assays?
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回答：
Dissolving S1023 in 15% Captisol is for oral gavage and it's a suspension.
