ホームページ Protein Tyrosine Kinase EGFR inhibitor - Autophagy activator Erlotinib For research use only.

Erlotinib

別名：CP358774, NSC 718781,OSI-774

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.

Erlotinib化学構造

CAS No. 183321-74-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 44500 国内在庫あり
JPY 103500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：sales@selleck.co.jp
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製品安全説明書

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99.99

Erlotinib関連製品

シグナル伝達経路

EGFR Signaling Pathways

EGFRシグナル伝達経路

EGFR阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
LLC Antitumor assay 100 mg/kg 14 days Antitumor activity against mouse LLC cells allografted in SCID mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd for 14 days 26188620
PC9 Antitumor assay 15 mg/kg 4 weeks Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse assessed as tumor regression at 15 mg/kg, qd measured after 4 weeks 26313252
PC9 Antitumor assay 15 mg/kg 4 weeks Antitumor activity against human PC9 cells expressing EGFR exon19 deletion mutant xenografted in mouse at 15 mg/kg, qd measured after 4 weeks 26313252
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生物活性

製品説明 Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Targets
EGFR [1]
(Cell-free assay)
2 nM
In Vitro
In vitro

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi human colon cancer cells and MDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi human colon cancer cells. [1] 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. [2] Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. [3] The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. [4] Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. [5]
Kinase Assay 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 colorimetric 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.
細胞実験 細胞株 A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells
濃度 30 nM-20 μM
反応時間 72 hours
実験の流れ

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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot Cleaved PARP / PARP P-Raf-1 / t-Raf-1 / p-MEK / t-MEK / p-ERK / t-ERK / p-PI3K / t-PI3K / p-AKT / AKT p-STAT3 / STAT3 / PTPMeg2 / p-EGFR / EGFR / pJAK2 / JAK2 / Bcl2 / Bcl-xl / Survivin 27508092
Immunofluorescence β-catenin E-cadherin / Vimentin 25209444
Growth inhibition assay Cell viability IC50 30377412
In Vivo
In Vivo

At doses of 100 mg/kg, Erlotinib HCl 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 HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate. [5]
動物実験 動物モデル Male 5-week-old BALB-nu/nu mice with HPAC cells
投与量 50 mg/kg
投与経路 Oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04172779 Not yet recruiting
Cirrhosis Liver
University of Texas Southwestern Medical Center|National Cancer Institute (NCI)
 July 2024 Phase 2
NCT06161558 Not yet recruiting
Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 1
NCT05827614 Recruiting
Non-small Cell Lung Cancer|Non-Small Cell Lung Adenocarcinoma|Non-Small Cell Squamous Lung Cancer|Head and Neck Squamous Cell Carcinoma|Esophageal Cancer|Gastric Cancer|Breast Cancer|Bladder Cancer|Ovarian Cancer|Endometrial Cancer|Liposarcoma
Boundless Bio
 March 24 2023 Phase 1
NCT03460678 Terminated
Carcinoma Non-Small-Cell Lung
Hikma Pharmaceuticals LLC
 February 28 2018 Phase 4

化学情報

分子量 393.44 化学式

C22H23N3O4
CAS No. 183321-74-6 SDF Download Erlotinib SDFをダウンロードする
Smiles COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (254.16 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 11 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機
Clear solution
5%DMSO 30% 5% 60%ddH2O
3.0mg/ml (7.63mM) Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 600 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil
0.55mg/ml (1.40mM) Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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よくある質問（FAQ）

質問1:
Can you please give me some advice for which solvent we should use to dissolve it for animal studies?

回答
For in vivo application, we recommend to use 5% DMSO+45% PEG 300+ddH2O up to 6mg/ml.

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