Gefitinib (ZD1839)

製品コードS1025

Gefitinib (ZD1839)化学構造

分子量(MW):446.90

Gefitinib (ZD-1839)は一種のEGFR阻害剤で、NR6wtEGFRとNR6Wの細胞中のTyr1173、Tyr992、Tyr1173とTyr992に作用する時のIC50値が37 nM、37nM、26 nMと57 nMにそれぞれ分かれることです。

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文献中の使用例(91)

カスタマーフィードバック(12)

  • Perturbation of EGFR by its ligand EGF and gefitinib (ZD-1839 Iressat; inhibits EGFR) produces opposite responses in the predicted EGFR target genes SOCS2 and NR2E1.

    Mol Syst Biol 2011 7, 486. Gefitinib (ZD1839) purchased from Selleck.

    Effects of shRNA-mediated RECK depletion on EGFR signaling in MEFs. (a) Immunoblotting (IB) of the indicated proteins in wild-type MEFs transduced with the indicated shRNAs and cultured for 48 h in the presence of 0.1% dimethyl sulfoxide (DMSO; vehicle) or 1 mM gefitinib (S1025, Selleck Chemicals,Houston, TX, USA). (b) Immunoprecipitation from whole lysates of cells from panel a with an anti-phosphorylated tyrosine (pTyr) antibody. Precipitates from 500 mg protein in whole cell lysates (upper) or 20 mg protein in whole cell lysates (lower) were analyzed by IB with anti-EGFR antibody.

    Oncogene 2010 30, 737-750. Gefitinib (ZD1839) 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 lM) 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 . Gefitinib (ZD1839) 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. Gefitinib (ZD1839) 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(4), 372-81. Gefitinib (ZD1839) purchased from Selleck.

    Suppression of EGFR signaling by Gefitinib is dose dependent and non- toxic at millimolar concentrations.Results from plaque reduction tests of Hep2 cells infected with VACV(12.5pfu/well) treated with a serial dilution of Gefitinib (1000-0.01 m) and analyzed for (A)proliferation as indicator of cytotoxicity,(B) IC50 of plaque size inhibition, (C)dose dependent inhibition of EGFR-ERK1/2signaling and VACV proteins by Western blot analysis (pEGFR detection was obtained from a different experiment with identicals ettings) and (D)dose dependent inhibition of orthopoxvirus genome replication by real-time PCR.Untreated VACV infectedcells and uninfected cells are shown as controls in the right panel.

    Antiviral Res 2010 89, 64-70. Gefitinib (ZD1839) purchased from Selleck.

  • A circular zone of EGFR activated but uninfected cells facilitate virus induced plaque development , efficiently blocked by Gefitinib. (A)Immun of luorescent staining of aplaque reduction tests with Hep2 cells 24,48,72 and 96 h after VACV infection (6.25pfu/chamber). VACV infected cells(green) were visualized by human IgG directed to orthopoxviruses (VIG) detected with a secondary FITC labelled antibody. Uninfected cells with activated EGFR signaling(red) are detected with a secondary Cy3labelled antibody. Positive cells for both , VACV and phosphorylated EGFR are shown in yellow(merge). Cellular nuclei are counterstained with DAPI. (B)Immunofluorescent staining of a plaque reduction test as described for (A) and treated with three different Gefitinib concentrations (1000 nM, 1 nM, and 0.01 nM) . The test was analyzed 96h afterVACV infection.Uninfected cells are shown as controls. Magnification100×.(For interpretation of the references to color in this figure legend , the reader is referred to the web version of the article.)

     

     

    Antiviral Res 2010 89, 64-70. Gefitinib (ZD1839) purchased from Selleck.

    The EGF-dependent increased association of PCM1 and AZI1 requires EGFR kinase activity. ZD1839 (Iressa)—EGFR tyrosine kinase inhibitor.

    Mol Biosyst 2011 7, 3223-33. Gefitinib (ZD1839) purchased from Selleck.

  • Reduction of GPER expression in HCC1806 cells after treatment with gefitinib. (A) Concentration dependence. HCC1806 cells were treated with 50-500 nM gefitinib for 48 h. GPER was detected by western blotting. (B) Time dependence. HCC1806 cells were treated with 200 nM gefitinib for 24-96 h. ap<0.05 vs. control; bp<0.001 vs. control. Mean values and SE of three independent experiments are shown. (C) Representative western blotting of concentration dependence. (D) Representative western blotting of time dependence

    Oncol Rep, 2017, 37(2):1212-1218. Gefitinib (ZD1839) purchased from Selleck.

    Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.

    Int J Proteomics 2011 215496. Gefitinib (ZD1839) purchased from Selleck.

  • Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of  Gefitinib for 24 hours.

     

     

    2010 Dr. Zhang of Tianjin Medical University. Gefitinib (ZD1839) purchased from Selleck.

    MTT assay result. 0-500nM Gefitinib treated with H1299, H358, H25 and HCC827 cell lines by 72h, Proliferation rate was tested.

     

     

    2010 Dr. Vicky Tin from University of Hong Kong. Gefitinib (ZD1839) purchased from Selleck.

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 Gefitinib (ZD-1839)は一種のEGFR阻害剤で、NR6wtEGFRとNR6Wの細胞中のTyr1173、Tyr992、Tyr1173とTyr992に作用する時のIC50値が37 nM、37nM、26 nMと57 nMにそれぞれ分かれることです。
特性 A potent EGFR tyrosine kinase inhibitor.
ターゲット
Tyr1173 (NR6W cells) [1] Tyr1173 (NR6wtEGFR cells) [1] Tyr992 (NR6wtEGFR cells) [1] Tyr992 (NR6W cells) [1]
26 nM 37 nM 37 nM 57 nM
体外試験

Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. [1] Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 nM. [2] The combination of Gefitinib (0.2 μM and 0.5 μM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone.. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB M2Txbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzieIhKSzVyPUCuNFU1KM7:TR?= NGLYR5YyPjVzNkS3Ny=>
NIH3T3 MVzGeY5kfGmxbjDBd5NigQ>? MUSwMlIh|ryP NVzubpJsOiCq MkniSG1UVw>? MYnJcohq[mm2aX;uJI9nKEWJRjDzeIlufWyjdHXkJIh2dWGwIHXyZmIyKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODF2NDFOwG0> NXPBcJBVOTZ2OECyPFQ>
COS7 NFTO[mZHfW6ldHnvckBCe3OjeR?= M{PEbFk3KM7:TR?= NIewNmhKdmirYnn0bY9vKG:oIHj1cYFvKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5Nm\A>? NG[xeG4yPzF5OEeyNi=>
A549 MmfPR5l1d3SxeHnjJGF{e2G7 MoPzPVYhcA>? M3rKNmROW09? MXXJR|UxRTF|LkW5JO69VQ>? MYmxPFMyOzhyNx?=
K562 NVm5dHhVS3m2b4TvfIlkKEG|c3H5 NIfW[GY6PiCq NX\oOIQ1TE2VTx?= M3PPeGlEPTB;OT6zOkDPxE1? MXexPFMyOzhyNx?=
MDA-MB-231 MoPRR5l1d3SxeHnjJGF{e2G7 NV;mS|kzQTZiaB?= M1X4[2ROW09? NGDGSpBKSzVyPUO2MlYyKM7:TR?= NXW4XVZqOTh|MUO4NFc>
MOLT4 M1nQSWN6fG:2b4jpZ{BCe3OjeR?= MWO5OkBp MV3EUXNQ MXXJR|UxRTF3LkCyJO69VQ>? NIXSd4QyQDNzM{iwOy=>
MCF7 NEPhTYxEgXSxdH;4bYMhSXO|YYm= Mn\xOVAh|ryP NFW3NnU4OiCq MnO2TWM2OD1zMj6wOUDPxE1? NWS5S3JmOTh5N{G4NVk>
BT474 NXrvSoFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWD0PI94PzJiaB?= MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNEe0JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWUQnKyJJdqfGhiRVO1NEBw\iByLkOg{txO M3TvVFE6ODJ6NEK0
HN5 NFnwdIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HnOVczKGh? Mmf5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkWgZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjD3bZRpKEWFNUCgc4YhOC5yMTFOwG0> MnSzNVkxOjh2MkS=
BA/F3 MY\DfZRwfG:6aXOgRZN{[Xl? MUm3NkBp NHzvUVREgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFXHSnIhVDh3OGKgcZV1[W62IIfpeIghUUN3MDDv[kAxNjBzMEig{txO M2\ON|E6OjN7MkK5
NIH3T3 M{PTO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3HRmM5PzJiaB?= MkPyS5Jwf3SqIHnubIljcXSrb36gc4YhdW:3c3WgUmlJNzOWMzDj[YxteyCneIDy[ZN{cW6pIHXyRlIh\2WwZTD3bZRpKEmFNUCgc4YhOC53NDFOwG0> MWSxPVY3PTN5Nx?=
MCF7 MX NWTMNodDTnWwY4Tpc44hSXO|YYm= NIjzTJE{OCCvaX6= Mof4TY5pcWKrdHnvckBw\iCEQ2LQJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMT6xJO69VQ>? MWSxPVk{Ojl4MB?=
A431 NWnnc|ZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mon2NVAh|ryP MXW3NkBp M1vEUmdKPTB;MD61NVQh|ryP MUixPVk3QTR4NR?=
A431 M3LCfGtqdmG|ZTDBd5NigQ>? M2X4WlAvOSEQvF2= NHXDTm0yKGh? MmPiTY5pcWKrdHnvckBw\iCHR1[tbY5lfWOnZDDFS2ZTKHCqb4PwbI9zgWyjdHnvci=> NHLubYkyQTl4OUS2OS=>
A431 M2PkV2tqdmG|ZTDBd5NigQ>? NWe5R4U{OTByIN88US=> MVuxNEBucW5? M4TlVHBzd2yxbnfl[EBqdmirYnn0c5J6KGGldHn2bZR6KG:oIFXHSk1qdmS3Y3XkJGVITlJicHjvd5Bpd3K7bHH0bY9v M{Hye|E6QTZ7NE[1
Sf9 NY\iUXh4U2mwYYPlJGF{e2G7 M3nVWVExKG2rbh?= Mn7MSG1UVw>? NXT2XY4{UW6qaXLpeIlwdiCxZjDFS2ZTKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHKnY3XweI9zKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODN|IN88US=> MmnCNlAxPTZ2MkW=
NCI-H1975 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH35NGY2KM7:TR?= NUXVPHg1PzJiaB?= NWL4[3d7UUN3ME24MlI3KM7:TR?= MojINlAyPTF4N{C=
NCI-H1975 MlrOT4lv[XOnIFHzd4F6 M2DKbFExKM7:TR?= NH7oOFlKdmirYnn0bY9vKG:oIFXHSnIh[XW2b4Doc5NxcG:{eXzheIlwdg>? NFPI[nozODF3MU[3NC=>
NCI-H1975 NVnuUVJZTnWwY4Tpc44hSXO|YYm= NVTsPJE4OTBizszN MnPNTY5pcWKrdHnvckBw\iCHUlLCNkBifXSxcHjvd5Bpd3K7bHH0bY9v M1PYbVIxOTVzNkew
NCI-H1975 Ml;lSpVv[3Srb36gRZN{[Xl? MWW1JO69VQ>? MU[0PEBp NHrJV5hKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHHzd4V{e2WmIHHzJIFkfGm4YYTpc44hd2ZiY3HzdIF{\S1| MWCyNFE2OTZ5MB?=
A375 NIfPToRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7WU|c1QCCq M{fL[WlEPTB;MkCuOVUh|ryP Mn\mNlA{ODR3M{e=
SMMC7721 M{G4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P0dFQ5KGh? MmG5TWM2OD1|Mz6xNkDPxE1? MlXiNlA{ODR3M{e=
DU145 M1HCfmN6fG:2b4jpZ{BCe3OjeR?= M3;RZVUh\A>? NXK1TXpJTE2VTx?= M3PkT2lEPTB;NEKuNVch|ryP MXiyNFQ3PjV3NR?=
MIAPaCa2 MonwR5l1d3SxeHnjJGF{e2G7 NWrt[Is3PSCm MonYSG1UVw>? NHXWTG9KSzVyPUWwMlYzKM7:TR?= MXWyNFQ3PjV3NR?=
PANC1 MYHDfZRwfG:6aXOgRZN{[Xl? NEjHUIk2KGR? MlHoSG1UVw>? NHXLbXhKSzVyPUSwMlQzKM7:TR?= NHu3TY4zODR4NkW1OS=>
PC9 MkO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXHSnIu\GWoaXPp[Y51KGi3bXHuJHBEQSClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wNVch|ryP Mn23NlEzODh6MEK=
PC9 NGK1[XhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPNZXg3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBoem:5dHitdoV{cXO2YX70JIh2dWGwIGDDPUBk\WyuczDlfJBz\XO|aX7nJGVITlJiRUe0On9CPzVyL2S3PVBOKG23dHHueEB4cXSqIFXDOVAhd2ZiNzFOwG0> NGfReY0zOTJyOEiwNi=>
PC3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxNEDPxE1? MkPVO|IhcA>? NEnEVHJFVVOR M2DBfGlEPTB;Nz60JO69VQ>? NYi1Z3p4OjF|NUO1OFY>
MDA-MB-468 M{fOS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HyXFExOCEQvF2= NGjJemw1QCCq NIHISZZFVVOR NIjHOFJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fS=> NVGwOnhGOjF2Mkm2N|I>
Plasmodium falciparum MVrxTHRUKHC{b3\pcIlv\yCob4KgbY5pcWKrdH;yd{Bw\iCSbHHzcY9lcXWvIH\hcINqeGG{dX2gdJJwdGmoZYLheIlwdg>? MlT1NlE5OTdyNEW=
NCI-H1993 M4LJbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIWwNY84OiCq M1PXS2ROW09? NFXvVmxKSzVyPUCuNUDPxE1? M3fmSVIyQTF4NEOz
NCI-H292 NUX6OHdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmiyO|IhcA>? NHPrXFRFVVOR M{fpWWlEPTB;MD6wNkDPxE1? NXLC[IlQOjF7MU[0N|M>
A431 M3rhS2tqdmG|ZTDBd5NigQ>? MlTENkBp MmXySG1UVw>? NXfYV3BpUW6qaXLpeIlwdiCxZjDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCHR1[td5RqdXWuYYTl[EBpfW2jbjDBOFMyKHerdHigTWM2OCCxZjCwMlAxOSEQvF2= MnjjNlIyODFzM{K=
MCF7 M33o[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{OzOVExOMLizsznM41N NGjkWIU1QCCq NUe1OopwTE2VTx?= MofERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKg[4Vv\SC5aYToJGlEPTBib3[gNVIvODVizszN MlrtNlIyOTlzM{C=
BT474 MoPaR5l1d3SxeHnjJGF{e2G7 NXjGS3Y6OTBizszN NUTCVmdKPDhiaB?= MVvDfZRwfG:6aXPpeJkh[WejaX7zeEB{\XK3bT3zeIFzfmWmIHj1cYFvKEKWNEe0JINmdGy| NVzibJV7OjJzM{izNFg>
MCF7 NVnsOZNSS3m2b4TvfIlkKEG|c3H5 MUCxNEDPxE1? NXXLb3pjPDhiaB?= M3LUTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHOncoXtMZN1[XK4ZXSgbJVu[W5iTVPGO{Bk\WyuczDveoVzNWW6cILld5NqdmdiRYLiRlIh[2WubIO= M2rmUlIzOTN6M{C4
HCC827 MorMT4lv[XOnIFHzd4F6 MmToNE4yOjVizszN NHjxbZkzPCCq NGfl[5BFVVOR MofkTY5pcWKrdHnvckBw\iCHR1\SJIRmdCCHN{S2MWE4PTBibYX0ZY51KFlzME[4JIF2fG:yaH;zdIhwenmuYYTpc44> NUjweJFzOjJ|M{mzOFI>
HCC827 NFOxWolMcW6jc3WgRZN{[Xl? Mn\yNE4yOjVizszN NEHXVlkzPCCq NYrMVoVVTE2VTx?= NXO0cnZoUW6qaXLpeIlwdiCxZjDFS2ZTKGSnbDDFO|Q3NUF5NUCgcZV1[W62LX3l[IlifGWmIFXyb{BxcG:|cHjvdplt[XSrb36= M2S0VFIzOzN7M{Sy
HCC827 MX\LbY5ie2ViQYPzZZk> NHXJWYMxNjF{NTFOwG0> MViyOEBp NGP0RXFFVVOR MXPJcohq[mm2aX;uJI9nKEWJRmKg[IVtKEV5NE[tRVc2OCCvdYThcpQudWWmaXH0[YQhSWu2IIDoc5NxcG:{eXzheIlwdg>? M2rRfVIzOzN7M{Sy
A431 NHzlZmFMcW6jc3WgRZN{[Xl? NWHN[mlpOTByIN88US=> MVGzNEBucW5? MnniTY5pcWKrdHnvckBw\iCHR1\SJIRmemm4ZXSg[pJwdSCqdX3hckBCPDNzIHPlcIwhdWWvYoLhcoUh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBxd2y7LVfseU1VgXJicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxMlA5KM7:TR?= MWWyNlY6QDd6Mh?=
H460 MYPDfZRwfG:6aXOgRZN{[Xl? M1LuWFczKGh? M4Dz[GlEPTB;NT61PUDPxE1? M4rWOFIzPzJ5NES5
HT-29 NXfD[G5GS3m2b4TvfIlkKEG|c3H5 MXy3NkBp M1[5e2lEPTB;Mz6zOkDPxE1? NUfLOoRrOjJ5Mke0OFk>
SGC7901 MUnDfZRwfG:6aXOgRZN{[Xl? NXrRVWI4PzJiaB?= MmnNTWM2OD1zMD6yOkDPxE1? NFrSXG8zOjd{N{S0PS=>
A498 M{H5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2OUigZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKGGwZDDTVmMhf2m2aDDJR|UxKG:oIEiuOkDPxE1? MnflNlI5OTh6NEi=
Calu3 M4X1[GN6fG:2b4jpZ{BCe3OjeR?= NHyzelAyOCEQvHevcWw> NWDKe4xDPzJiaB?= NVGxXoxjUUN3ME2xMlYh|ryP NHfnPGUzOzFzNkG2PC=>
FADU NGPlOmtEgXSxdH;4bYMhSXO|YYm= MYSxNEDPxGdxbVy= MV:3NkBp M1rhZWlEPTB;MD6wOUDPxE1? NHewO5ozOzFzNkG2PC=>
HCC827 M3H6cWN6fG:2b4jpZ{BCe3OjeR?= M2fCUFExKM7:Zz;tUC=> M37kN|czKGh? NX3STIdPUUN3ME2wMlAxOTVizszN NVzYTG1kOjNzMU[xOlg>
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ES4 NH7XR3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrENms6UUN3ME2zMlgzOjh4IN88US=> MoLsV2FPT0WU
NCI-H28 M3rPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV76UoU5UUN3ME2zMlgzQTZzIN88US=> M1fqbnNCVkeHUh?=
NCI-H1155 NGX3UXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPGWYJLUUN3ME2zMlg1OTV7IN88US=> NYW4TFJXW0GQR1XS
KURAMOCHI MlzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLoepZVUUN3ME2zMlg3ODV4IN88US=> NV[xW5RIW0GQR1XS
NCI-H69 M2fNcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:zTFNKSzVyPUOuPVAyPzhizszN MWLTRW5ITVJ?
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JVM-2 NX3mOIJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrpVmFDUUN3ME2zMlk1PzV{IN88US=> M4jGSXNCVkeHUh?=
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TCCSUP MkfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;nfWlEPTB;ND6xNVA2KM7:TR?= M2K2dnNCVkeHUh?=
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EW-11 NH3PfGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7GeI9uUUN3ME20MlE{OjZzIN88US=> MmPlV2FPT0WU
KARPAS-299 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELiU41KSzVyPUSuN|ExOTNizszN NVPv[5pVW0GQR1XS
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SK-OV-3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;jTWM2OD12LkS2NFQzKM7:TR?= NVWxfpNDW0GQR1XS
A172 NHL4WY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXlTWM2OD12LkW1OVIyKM7:TR?= Mn\hV2FPT0WU
NB10 Mm\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrUW2VKSzVyPUSuOVk4QDFizszN Mon3V2FPT0WU
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KYSE-520 M3n5[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTRwOEiwNVgh|ryP NX\O[WQ2W0GQR1XS
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TE-9 NEDTOFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfJcHY2UUN3ME21MlAyPTJ3IN88US=> MmTDV2FPT0WU
NCI-H1838 NH;OU2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfuPVYzUUN3ME21MlAzODd4IN88US=> MV3TRW5ITVJ?
KP-N-YN MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\QTHJKSzVyPUWuNVI2QTFizszN NHfye3NUSU6JRWK=
ALL-PO Mk\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjR[2VsUUN3ME21MlIzPTh5IN88US=> M3nKd3NCVkeHUh?=
NOMO-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3T3TGlEPTB;NT6yN|E4PiEQvF2= NHjpN21USU6JRWK=
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ATN-1 NGC4d3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXu1bIZPUUN3ME21MlQyOTh2IN88US=> MoDDV2FPT0WU
AGS MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTVwNEm2NVgh|ryP NUDzV41TW0GQR1XS
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RT-112 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTVwOUCyOFUh|ryP M2X6b3NCVkeHUh?=
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Mewo NGj5XlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTZwMUG0PFch|ryP M1rIZXNCVkeHUh?=
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8-MG-BA MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTZwMUmzO|kh|ryP MXrTRW5ITVJ?
SK-MEL-28 NHj0RWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LYbmlEPTB;Nj6yNFk3PyEQvF2= NUDKb4RTW0GQR1XS
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CAL-120 NHvhcmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfpfG9QUUN3ME22MlQ2OTZ{IN88US=> NXrEVWw1W0GQR1XS
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GCT MoOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoP4TWM2OD14LkWzN|g4KM7:TR?= MYjTRW5ITVJ?
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SK-HEP-1 M3P1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HFSGlEPTB;Nj63NVc2OyEQvF2= MYTTRW5ITVJ?
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NB12 MkHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP1XYhKSzVyPU[uO|g1ODRizszN MVTTRW5ITVJ?
A388 NWfafGV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWruWnZkUUN3ME22Mlg6PTJizszN MV3TRW5ITVJ?
KLE NV;4WHZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HEd2lEPTB;Nj65OlUyPiEQvF2= MlTIV2FPT0WU
TE-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XZO2lEPTB;Nz6wOFk3PyEQvF2= M1;x[nNCVkeHUh?=
NCI-H2405 NFjv[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\mTWM2OD15LkC4N|k{KM7:TR?= M1fZWnNCVkeHUh?=
OVCAR-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j2W2lEPTB;Nz6xOVM2KM7:TR?= NVj0dYJSW0GQR1XS
KP-N-YS MofzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Xtd2lEPTB;Nz6xPFE1KM7:TR?= NYD4T5BwW0GQR1XS
NOS-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTdwMkW4Nlgh|ryP MoPnV2FPT0WU
DMS-114 NFe0NmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTdwMkm2N|Eh|ryP MUHTRW5ITVJ?
NCI-H2030 NVmxd2t[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTdwM{O2PVgh|ryP NFPNOItUSU6JRWK=
HEL MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTdwM{e1NlEh|ryP MWjTRW5ITVJ?
CAL-62 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqzXmJKSzVyPUeuN|k5PjZizszN MljtV2FPT0WU
COLO-668 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mom5TWM2OD15LkSzPVY4KM7:TR?= M4TDV3NCVkeHUh?=
SKG-IIIa NXvj[HRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoG3TWM2OD15LkS1N|gyKM7:TR?= MkGxV2FPT0WU
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NB14 MlrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTN6LkS1OFQh|ryP NWTLWYttW0GQR1XS
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NCI-H510A NHjn[m1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\sXWlEPTB;M{iuOlQ2OSEQvF2= M4LkPHNCVkeHUh?=
NMC-G1 M{fEU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jsR2lEPTB;M{iuO|IzOiEQvF2= M1jYWHNCVkeHUh?=
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MFM-223 NYHsPHd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzBcmlKSzVyPUO4Mlk1OzFizszN NXXCXWNDW0GQR1XS
PAN1 M3PDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnwU|NKSzVyPUO4Mlk6OTlizszN Mo\OV2FPT0WU
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COLO-679 NILIdINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzOTWM2OD1|OT65O|A5KM7:TR?= NHizfXhUSU6JRWK=
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SNU-387 Ml3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;PTWM2OD12MD64NlM5KM7:TR?= NFmxXVZUSU6JRWK=
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G-402 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\rTWM2OD12MT6wPFA6KM7:TR?= MXzTRW5ITVJ?
MZ1-PC NXzLV2pvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTRzLkixJO69VQ>? MmPjV2FPT0WU
SW1417 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17nUWlEPTB;NEKuN|A{KM7:TR?= M125R3NCVkeHUh?=
RERF-LC-MS NYPRV4Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfyTWM2OD12Mj61NFg4KM7:TR?= MmfyV2FPT0WU
SF539 NV36S5hIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXSTWM2OD12Mj61OVI6KM7:TR?= MnfYV2FPT0WU
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RO82-W-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjvfGJKSzVyPUSzMlYyPTNizszN M{HzUHNCVkeHUh?=
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SW756 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XnbGlEPTB;NEOuPFI1OiEQvF2= M{fROHNCVkeHUh?=
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H-EMC-SS NEXxcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnLUWR{UUN3ME20OU44Pjl|IN88US=> NGXQOWFUSU6JRWK=
NCI-H2052 M1;pd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3sTWM2OD12NT65NFI4KM7:TR?= M3S0XXNCVkeHUh?=
SW684 NHvtNIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjHZVh6UUN3ME20O{4xODhzIN88US=> M4Dad3NCVkeHUh?=
HCC1569 M{L3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPmTWM2OD12Nz6xOlU5KM7:TR?= NF32NmlUSU6JRWK=
KGN NFLlXZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTR5LkOzNVEh|ryP MmWxV2FPT0WU
LCLC-103H MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rCSGlEPTB;NEeuOFQxPCEQvF2= Mk\FV2FPT0WU
SW780 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrwfI1HUUN3ME20O{43OzVzIN88US=> MV\TRW5ITVJ?
NCI-H1703 NUXlTVBvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1q2SGlEPTB;NEiuN|M2OiEQvF2= NHjOXWRUSU6JRWK=
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多くの細胞株試験データを見る場合、クリックしてください

体内試験 Gefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. [3] Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment. [4]

お薦めの試験操作(参考用のみ)

細胞試験: [1]
+ 展開
  • 細胞株: NR6, NR6M and NR6W cells
  • 濃度: 0-2 μM
  • 反応時間: 72 hours
  • 実験の流れ: Exponentially growing cells including NR6, NR6M, NR6M and NR6W cells are seeded in sextuple in 96-well plates at a concentration of 2000 cells/well, allowed to adhere and subsequently washed in PBS and incubated overnight in medium containing 0.5% FCS. Cells are then treated with varying concentrations (0-2 μM) of Gefitinib or the solute control DMSO and EGF. The optimal EGF concentration for inducing proliferation of NR6wtEGFR and NR6W cells has previously been determined and hence NR6wtEGFR and NR6W cells are supplemented with 10 nM and 0.1 nM EGF, respectively. EGF is not added to NR6 and NR6M cells. After 72 hours the amount of cells are measured by performing a MTT proliferation assay.
    (参考用のみ)
動物試験:[3]
+ 展開
  • 動物モデル: Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells.
  • 製剤: 0.5% polysorbate
  • 投薬量: 100 mg/kg
  • 投与方法: Once daily by oral administration (0.1 mL/10 g body weight) for 14 days
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 89 mg/mL (199.14 mM)
Ethanol 4 mg/mL (8.95 mM)
Water Insoluble
体内 順序で溶剤を入れること:
1% CMC Na
30mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 446.90
化学式

C22H24ClFN4O3

CAS No. 184475-35-2
保管
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03050164 Completed Bioequivalence Study Hunan Kelun Pharmaceutical Co., Ltd. September 8, 2016 Phase 1
NCT02856893 Not yet recruiting NSCLC European Organisation for Research and Treatment of Cancer - EORTC|AstraZeneca March 2017 Phase 2
NCT02976116 Recruiting NSCLC Hutchison Medipharma Limited December 2016 Phase 2
NCT02951637 Not yet recruiting Lung Adenocarcinoma Shanghai Chest Hospital|Ruijin Hospital|Changhai Hospital December 2016 Phase 2
NCT02930954 Not yet recruiting Non-small-cell Lung Cancer Caicun Zhou|Tongji University November 2016 Phase 2
NCT02929693 Enrolling by invitation Cancer Shanghai University of Traditional Chinese Medicine|Shanghai Chest Hospital|Shanghai Pulmonary Hospital, Shanghai, China October 2016 Phase 3

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    I try to dissolve Gefitinib (ZD1839) in 0.5% methylcellulose+0.2% Tween 80 for in vivo experiments. However, when I prepare the mixture, it forms precipitates. Exists another way to dissolve completely the compound?

  • 回答:

    S1025 can be dissovled in both 5% DMSO+corn oil and 5% DMSO+30% PEG 300+5% Tween 80+ddH2O at 2.5 mg/ml clearly. It dissolves in DMSO not readily, please sonicate and warm it in water bath at about 45 degree, and dissolve it clearly first. Then add other solvent.

EGFR信号経路図

EGFR Inhibitors with Unique Features

相関EGFR製品

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID