Erlotinib HCl (OSI-744)

目录号:S1023 别名: (CP358774, NSC 718781) HCl

Erlotinib HCl (OSI-744) Chemical Structure

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。

规格 价格 库存 购买数量  
RMB 1183.19 现货
RMB 3012.92 现货


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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.

  • 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.

  • (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.

  • 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.

  • 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.

  • 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.

  • 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.

  • 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.

  • 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。
(Cell-free assay)
2 nM

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A431 cells MlrLSpVv[3Srb36gZZN{[Xl? M1HQfGlvcGmkaYTpc44hd2ZiRVfGVkBqdiCqdX3hckBCPDNzIHPlcIx{KGK7IFjUVmYh[XO|YYmsJGlEPTB;MD60NkDPxE1w M{HYfVE6QDF3NEGy

... Click to View More Cell Line Experimental Data

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。


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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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  • Cell lines: HPAC细胞系和Capan-1细胞
  • Concentrations: 0.01 μM-10 μM
  • Incubation Time: 4天或6天
  • Method: 为了测评对细胞增殖的抑制作用,进行MTT实验。细胞在96孔板上在37oC下预温育,单独加入Erlotinib 和Gemcitabine,或者联合加入。在37oC下处理4天(HPAC细胞)或6天(Capan-1 细胞)后,每孔加入10 mL MTT,然后在37oC下温育2-5小时。使用Benchmark Plus 酶标仪在450和600 nm处测定每孔的光密度。每组每种药物实验独立重复进行2次或3次。按如下计算细胞增殖抑制百分数: [(药物处理孔中的平均吸光值-无细胞孔中平均吸光值)/(对照组孔中平均吸光值-无细胞孔中平均吸光值)] × 100。
    (Only for Reference)
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  • Animal Models: 携带HPAC细胞的雄性5周大的BALB-nu/nu小鼠
  • Formulation: 6% Captisol
  • Dosages: 50 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 4 mg/mL warmed (9.3 mM)
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。


分子量 429.90


CAS号 183319-69-9
稳定性 powder
in solvent
别名 (CP358774, NSC 718781) HCl





质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)


  • 质量

*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。




开始浓度 x 开始体积 = 最终浓度 x 最终体积


稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1

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。.


  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2


质量 浓度 体积 分子量


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 --





  • * 必填项


  • 问题 1:

    Whether S1023 is suitable for mouse assays?

  • 回答:

    Dissolving S1023 in 15% Captisol is for oral gavage and it's a suspension.

EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features


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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID