Erlotinib (OSI-774) HCl

製品コード:S1023 別名:CP358774, NSC 718781

For research use only.

Erlotinib (OSI-774, CP358774, NSC 718781) HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

Erlotinib (OSI-774) HCl化学構造

CAS No. 183319-69-9

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 33700
JPY 26400
JPY 63400

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(509)

製品安全説明書

EGFR阻害剤の選択性比較

相関EGFR製品

生物活性

製品説明 Erlotinib (OSI-774, CP358774, NSC 718781) HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
ターゲット
HER1/EGFR [1]
(Cell-free assay)
2 nM
体外試験

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi humancolon 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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SKBR3 cells NEf2NnRHfW6ldHnvckBie3OjeR?= NVLYXGdiUW6qaXLpeIlwdiCxZjDISXIzKGmwIHj1cYFvKFONQmKzJINmdGy|IHL5JGhVWkZiYYPzZZktKEmFNUC9NU45QSEQvF2u Mnv0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6MUW0NVIoRjF7OEG1OFEzRC:jPh?=
human A431 cells MV7GeY5kfGmxbjDhd5NigQ>? MXLJcohq[mm2aX;uJI9nKEWJRmKgbY4hcHWvYX6gRVQ{OSClZXzsd{BjgSCKVGLGJIF{e2G7LDDJR|UxRTBwNEKg{txONg>? NE\XUnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUixOVQyOid-MUm4NVU1OTJ:L3G+
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MCF7 NFTYNm5EgXSxdH;4bYNqfHliYYPzZZk> NWHDPI5vS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTVJvcH;zbZRqfmViTVPGO{Bk\WyuczygTWM2OCB;IECuNFAyOiEQvF2u M364flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEmwOlUzLz5{NEi5NFY2OjxxYU6=
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NCI-H1975 NIHNW2lCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1rlNFczKGi{cx?= NHXZW|lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOTl5NTDj[YxteyCneIDy[ZN{cW6pIFXHSnIhXDd7MF2gcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB4Lkmg{txONg>? NFyzZ|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG4N|c1Oid-MkSxPFM4PDJ:L3G+
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NCI-H1975 M4nx[WN6fG:2b4jpZ4l1gSCjc4PhfS=> MVW0PEBpenN? M{XtcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5EUS2KMUm3OUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iNz60PVgh|ryPLh?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEizNEc,OjR7MEC4N|A9N2F-
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OVCAR-4 NV7nTIxET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkXJTWM2OCB;IEiuPFQzOTlizszN MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVMwLz6VQV7HSXI9N2F-
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アッセイ
Methods Test Index PMID
Western blot p-Met / Met / p-Axl / Axl / pERK / ERK / pEGFR / EGFR / p-STAT3 / STAT3 / p-Akt / Akt ; p-Raf-1 / Raf-1 / p-MEK / MEK ; cleaved PARP / PARP ; p27 / pS10-p27 / pT157-p27 / pT187-p27 ; Bcl-2 / Bcl-xl / Mcl-1 / Bax / Bak / Bad / Bim EL / PUMA 28604685 27508092 21045138 17927446
Immunofluorescence Bax / Cyto C ; E-cadherin / β-catenin / Vimentin ; EGFR 17927446 19825949 27612423
Growth inhibition assay Cell viability 30377412
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
  • 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.

細胞試験:[2]
  • 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.
動物試験:[6]
  • 動物モデル:Male 5-week-old BALB-nu/nu with HPAC cells
  • 投薬量:50 mg/kg
  • 投与方法:Oral administration

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
15% Captisol
混合させたのち直ちに使用することを推奨します。

16 mg/mL warmed (suspension)

化学情報

分子量 429.90
化学式

C22H23N3O4.HCl

CAS No. 183319-69-9
Storage 3年 -20°C
2年 -80°C in solvent
Smiles COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl

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

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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質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04172779 Not yet recruiting Drug: Erlotinib Hydrochloride Cirrhosis Liver University of Texas Southwestern Medical Center July 2022 Phase 2
NCT03460678 Terminated Drug: Pemetrexed|Drug: Erlotinib Carcinoma Non-Small-Cell Lung Hikma Pharmaceuticals LLC February 28 2018 Phase 4
NCT02942095 Active not recruiting Drug: Ixazomib|Drug: Erlotinib Solid Tumors M.D. Anderson Cancer Center|Millennium: The Takeda Oncology Company March 6 2017 Phase 1
NCT02991651 Suspended Drug: IRX4204|Drug: erlotinib Lung Cancer Nonsmall Cell Io Therapeutics|Dartmouth College May 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

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よくある質問(FAQ)

質問1:
Whether S1023 is suitable for mouse assays?

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

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