Gefitinib (ZD1839)

製品コードS1025

Gefitinib (ZD1839)化学構造

分子量(MW):446.90

Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

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JPY 31706.00
JPY 24402.00
JPY 44820.00

文献中Selleckの製品使用例(95)

カスタマーフィードバック(14)

  • c, HCC4006 lung cancer cells that have acquired a high-mesenchymal state concomitant with becoming resistant to gefitinib (red curve) exhibit increased sensitivity to GPX4 inhibition.

    Nature, 2017, 547(7664):453-457. Gefitinib (ZD1839) purchased from Selleck.

    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.

    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.

    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.

  • Inhibition of 5-HT-induced 5-HT3A and 5-HT3AB receptor currents.

    Eur J Pharmacol, 2017, 821:21-28. 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) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.
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 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DvfGlEPTB;MD6wOVQh|ryP M{DTZVE3PTF4NEez
NIH3T3 MmL0SpVv[3Srb36gRZN{[Xl? MXOwMlIh|ryP NFTlbZgzKGh? MYDEUXNQ NXrFNppPUW6qaXLpeIlwdiCxZjDFS2Yhe3SrbYXsZZRm\CCqdX3hckBmemKEMTDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxOFQh|ryP NGTwUo0yPjR6MEK4OC=>
COS7 M2XWO2Z2dmO2aX;uJGF{e2G7 NHr4TXA6PiEQvF2= Mm\jTY5pcWKrdHnvckBw\iCqdX3hckBLSUt{IG[2NVdHKG23dHHueEBmgHC{ZYPz[YQ> M{D2OVE4OTd6N{Ky
A549 NGjmZmJEgXSxdH;4bYMhSXO|YYm= NE\BVJg6PiCq NXnO[FBGTE2VTx?= Mn\iTWM2OD1zMz61PUDPxE1? MmnuNVg{OTN6MEe=
K562 NE\DNpVEgXSxdH;4bYMhSXO|YYm= MnXnPVYhcA>? M1\xfGROW09? MWrJR|UxRTlwM{[g{txO NIr1UWMyQDNzM{iwOy=>
MDA-MB-231 NXf1XZVPS3m2b4TvfIlkKEG|c3H5 NH6ycpg6PiCq MWfEUXNQ MYrJR|UxRTN4Lk[xJO69VQ>? NGPEclIyQDNzM{iwOy=>
MOLT4 MV;DfZRwfG:6aXOgRZN{[Xl? NITUZ3Q6PiCq MoXXSG1UVw>? NXXXXYNyUUN3ME2xOU4xOiEQvF2= NIToOGcyQDNzM{iwOy=>
MCF7 M3TjXmN6fG:2b4jpZ{BCe3OjeR?= NHPDXoY2OCEQvF2= MnrvO|IhcA>? MVjJR|UxRTF{LkC1JO69VQ>? MWixPFc4OThzOR?=
BT474 MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:3NkBp NVz5W5BNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFQ4PCClZXzsd{BwfmW{ZYjwdoV{e2mwZzDFVmJjOiC5aYToJGVEPTBib3[gNE4{KM7:TR?= MXixPVAzQDR{NB?=
HN5 MoO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz6fHR2PzJiaB?= M4LhcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKge4l1cCCHQ{WwJI9nKDBwMEGg{txO MnnpNVkxOjh2MkS=
BA/F3 M1LwXWN6fG:2b4jpZ{BCe3OjeR?= MU[3NkBp Mn7NR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCHR1\SJGw5PTiUIH31eIFvfCC5aYToJGlEPTBib3[gNE4xOTB6IN88US=> M2iz[lE6OjN7MkK5
NIH3T3 M{\NWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWC3NkBp MY\Hdo94fGhiaX7obYJqfGmxbjDv[kBud3W|ZTDOTWgwO1R|IHPlcIx{KGW6cILld5NqdmdiZYLCNkBo\W6nIIfpeIghUUN3MDDv[kAxNjV2IN88US=> MnjhNVk3PjV|N{e=
MCF7 MX M{XBb2Z2dmO2aX;uJGF{e2G7 MmK0N|AhdWmw NXr6RnhQUW6qaXLpeIlwdiCxZjDCR3JRKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNU4yKM7:TR?= MkPyNVk6OzJ7NkC=
A431 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL5WmMyOCEQvF2= M33mZVczKGh? NXXQRmQ6T0l3ME2wMlUyPCEQvF2= NEDDTYoyQTl4OUS2OS=>
A431 MoW1T4lv[XOnIFHzd4F6 NV;iOmpOOC5zIN88US=> NUnOcFh7OSCq MXnJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;u NHLJVIMyQTl4OUS2OS=>
A431 NFLSd4ZMcW6jc3WgRZN{[Xl? MkjqNVAxKM7:TR?= Ml7MNVAhdWmw NFX6d5VRem:ub37n[YQhcW6qaXLpeI9zgSCjY4Tpeol1gSCxZjDFS2YucW6mdXPl[EBGT0[UIIDoc5NxcG:{eXzheIlwdg>? MnHONVk6Pjl2NkW=
Sf9 MUnLbY5ie2ViQYPzZZk> Mkf3NVAhdWmw NX7ie4ZqTE2VTx?= NHPOU2FKdmirYnn0bY9vKG:oIFXHSnIh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhemWlZYD0c5Ih[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzNizszN MW[yNFA2PjR{NR?=
NCI-H1975 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHidVk2KM7:TR?= Mk\VO|IhcA>? M2\HNWlEPTB;OD6yOkDPxE1? NV2ySndOOjBzNUG2O|A>
NCI-H1975 NIrmZ2tMcW6jc3WgRZN{[Xl? MoXYNVAh|ryP NWPwNlFHUW6qaXLpeIlwdiCxZjDFS2ZTKGG3dH;wbI9{eGixconsZZRqd25? NF[xe5YzODF3MU[3NC=>
NCI-H1975 NUPQSo1bTnWwY4Tpc44hSXO|YYm= M33kZ|ExKM7:TR?= NFG2WXJKdmirYnn0bY9vKG:oIFXSRmIzKGG3dH;wbI9{eGixconsZZRqd25? NYf4OIt3OjBzNUG2O|A>
NCI-H1975 M4GydWZ2dmO2aX;uJGF{e2G7 NEHKO3k2KM7:TR?= MlTTOFghcA>? MX3JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGG|c3Xzd4VlKGG|IHHjeIl3[XSrb36gc4Yh[2G|cHHz[U0{ M1jzR|IxOTVzNkew
A375 NX3rZ3dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDyRmNTPDhiaB?= Mnm5TWM2OD1{MD61OUDPxE1? NFTEfY4zODNyNEWzOy=>
SMMC7721 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HFeFQ5KGh? NUGye3dPUUN3ME2zN{4yOiEQvF2= NFTaWIczODNyNEWzOy=>
DU145 NILsXlVEgXSxdH;4bYMhSXO|YYm= NX\SdW5kPSCm NHPRd4pFVVOR MlX6TWM2OD12Mj6xO{DPxE1? NY\mNnpuOjB2Nk[1OVU>
MIAPaCa2 NEjnNFlEgXSxdH;4bYMhSXO|YYm= NWDa[INSPSCm MYfEUXNQ MVfJR|UxRTVyLk[yJO69VQ>? M4X3SlIxPDZ4NUW1
PANC1 NWTweII6S3m2b4TvfIlkKEG|c3H5 MWG1JIQ> MVvEUXNQ MX\JR|UxRTRyLkSyJO69VQ>? MonyNlA1PjZ3NUW=
PC9 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXHSnIu\GWoaXPp[Y51KGi3bXHuJHBEQSClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wNVch|ryP Mo\VNlEzODh6MEK=
PC9 M2TPWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDndo94fGhvcnXzbZN1[W62IHj1cYFvKFCFOTDj[YxteyCneIDy[ZN{cW6pIFXHSnIhTTd2Nm;BO|UxN1R5OUDNJI12fGGwdDD3bZRpKEWFNUCgc4YhPyEQvF2= NIrONZMzOTJyOEiwNi=>
PC3 M17iN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13WN|ExKM7:TR?= NHHZcos4OiCq MmfNSG1UVw>? NYHhRZFMUUN3ME23MlQh|ryP NYHSZppCOjF|NUO1OFY>
MDA-MB-468 M3jU[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2K1ZlExOCEQvF2= M4jUOFQ5KGh? M2XTR2ROW09? M3jiOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5 M{ixNlIyPDJ7NkOy
Plasmodium falciparum Mnj4dWhVWyCycn;mbYxqdmdiZn;yJIlvcGmkaYTvdpMhd2ZiUHzhd41w\Gm3bTDmZYxkcXCjcoXtJJBzd2yrZnXyZZRqd25? Mme0NlE5OTdyNEW=
NCI-H1993 NULwenlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWe3NkBp MWTEUXNQ MWPJR|UxRTBwMTFOwG0> M4ftOVIyQTF4NEOz
NCI-H292 NV;rO3ZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fYUVczKGh? MUnEUXNQ MlnXTWM2OD1yLkCyJO69VQ>? NWOyOYdZOjF7MU[0N|M>
A431 NIC3coFMcW6jc3WgRZN{[Xl? NUPoXZpmOiCq NG[5RVFFVVOR MlL5TY5pcWKrdHnvckBw\iCHR1\SJJBpd3OyaH;yfYxifGmxbjDpckBGT0Zvc4TpcZVt[XSnZDDoeY1idiCDNEOxJJdqfGhiSVO1NEBw\iByLkCwNUDPxE1? MVKyNlExOTF|Mh?=
MCF7 M{LGb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjiVJBNOTBywrFOwIcwdUx? M{Xk[FQ5KGh? NYnFSFMxTE2VTx?= NGfMXGJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgc5ZmemW6cILld5NqdmdiRVfGVkBo\W6nIIfpeIghUUN3MDDv[kAyOi5yNTFOwG0> M3XIRlIzOTF7MUOw
BT474 M3;0[GN6fG:2b4jpZ{BCe3OjeR?= NULEenp4OTBizszN MYG0PEBp NVnKWFQ6S3m2b4TvfIlkcXS7IHHnZYlve3Ric3XyeY0ue3Sjco\l[EBpfW2jbjDCWFQ4PCClZXzsdy=> MU[yNlE{QDNyOB?=
MCF7 NUPRWFl4S3m2b4TvfIlkKEG|c3H5 NU\vVGFyOTBizszN MUO0PEBp NF;K[YtEgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIF3DSlch[2WubIOgc5Zmei2neIDy[ZN{cW6pIFXyZmIzKGOnbHzz MWGyNlE{QDNyOB?=
HCC827 M4rZdWtqdmG|ZTDBd5NigQ>? NG\wOW4xNjF{NTFOwG0> NH;ielUzPCCq NFyzfVJFVVOR M4C3b2lvcGmkaYTpc44hd2ZiRVfGVkBl\WxiRUe0Ok1CPzVyIH31eIFvfCC\MUC2PEBifXSxcHjvd5Bpd3K7bHH0bY9v MX:yNlM{QTN2Mh?=
HCC827 Mme1T4lv[XOnIFHzd4F6 NVruUJdiOC5zMkWg{txO NVGxPW43OjRiaB?= MV;EUXNQ MX;Jcohq[mm2aX;uJI9nKEWJRmKg[IVtKEV5NE[tRVc2OCCvdYThcpQudWWmaXH0[YQhTXKtIIDoc5NxcG:{eXzheIlwdg>? M4exTFIzOzN7M{Sy
HCC827 MoLnT4lv[XOnIFHzd4F6 NHy2cIMxNjF{NTFOwG0> M2LEeFI1KGh? NHe5emFFVVOR NIW1[XdKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRvbXXkbYF1\WRiQXv0JJBpd3OyaH;yfYxifGmxbh?= NEfkV2kzOjN|OUO0Ni=>
A431 NWO5cGV7U2mwYYPlJGF{e2G7 NIez[HcyODBizszN NGH1V5g{OCCvaX6= NYfRV5ZNUW6qaXLpeIlwdiCxZjDFS2ZTKGSncnn2[YQh\nKxbTDoeY1idiCDNEOxJINmdGxibXXtZpJidmViYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCyb3z5MWdtfS2WeYKgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAyNjB6IN88US=> M4PPO|IzPjl6N{iy
H460 NVfzR4JNS3m2b4TvfIlkKEG|c3H5 NIf5PWQ4OiCq MVPJR|UxRTVwNUmg{txO NWPPTGxGOjJ5Mke0OFk>
HT-29 NFjhSZdEgXSxdH;4bYMhSXO|YYm= M2\6XlczKGh? NGK3XJZKSzVyPUOuN|Yh|ryP NIfa[HgzOjd{N{S0PS=>
SGC7901 MVjDfZRwfG:6aXOgRZN{[Xl? Mo\HO|IhcA>? M1nENGlEPTB;MUCuNlYh|ryP MUGyNlczPzR2OR?=
A498 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfyVmZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0PVgh[2WubIOg[ZhxemW|c3nu[{BGT0[UIHHu[EBUWkNid3n0bEBKSzVyIH;mJFgvPiEQvF2= NFHZb48zOjhzOEi0PC=>
Calu3 MnLMR5l1d3SxeHnjJGF{e2G7 NWT4SodrOTBizsznM41N MXq3NkBp M4nCWWlEPTB;MT62JO69VQ>? MofsNlMyOTZzNki=
FADU M2jXXWN6fG:2b4jpZ{BCe3OjeR?= MlHkNVAh|rypL33M MnriO|IhcA>? NY\Jc41KUUN3ME2wMlA2KM7:TR?= NHrjdIYzOzFzNkG2PC=>
HCC827 NFHiOmlEgXSxdH;4bYMhSXO|YYm= MYKxNEDPxGdxbVy= MUW3NkBp NVjmfpE{UUN3ME2wMlAxOTVizszN MljoNlMyOTZzNki=
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Sf9 MoHyT4lv[XOnIFHzd4F6 NF;lNZoyKGh? NUDKc5lpTE2VTx?= MoPITY5pcWKrdHnvckBw\iCqdX3hckBIW1RvdHHn[4VlKEWJRmKgUFg{PFJibYX0ZY51KGW6cILld5Nm\CC5aYToJGlEPTBib3[gNE4xOTVizszN NHvtNJQzOzZzMU[5NS=>
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VA-ES-BJ NVjs[nRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXflbGVDUUN3ME22MlMxPDZ{IN88US=> M4DiWnNCVkeHUh?=
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GCT M3;MUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\MfWlEPTB;Nj61N|M5PyEQvF2= M4fOWHNCVkeHUh?=
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SK-HEP-1 NV7RS3V{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\VW25DUUN3ME22MlcyPzV|IN88US=> NEPmPWhUSU6JRWK=
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DMS-114 NFG2SYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17tfWlEPTB;Nz6yPVY{OSEQvF2= M{XQbnNCVkeHUh?=
NCI-H2030 MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnNOIpHUUN3ME23MlM{Pjl6IN88US=> NWrpUGFsW0GQR1XS
HEL M3zYVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXsZ5JYUUN3ME23MlM4PTJzIN88US=> NHPtN4hUSU6JRWK=
CAL-62 M1Ll[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jOdWlEPTB;Nz6zPVg3PiEQvF2= NF;DTnFUSU6JRWK=
COLO-668 M{Kx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\oTWM2OD15LkSzPVY4KM7:TR?= NHKzOopUSU6JRWK=
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HCC1419 NEjkWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LURWlEPTB;Nz60Olg{OyEQvF2= NWfqZmN5W0GQR1XS
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NB14 NF\WR45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3f1cWlEPTB;M{iuOFU1PCEQvF2= M{fjRXNCVkeHUh?=
D-423MG MljZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3XTWM2OD1|OD60PFY6KM7:TR?= Mn72V2FPT0WU
NCI-H510A MonkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPscmNTUUN3ME2zPE43PDVzIN88US=> M2jV[XNCVkeHUh?=
NMC-G1 NHfxUYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTN6LkeyNlIh|ryP NHn6PWxUSU6JRWK=
SW948 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fDWGlEPTB;M{iuPFk1QSEQvF2= MX;TRW5ITVJ?
MFM-223 Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe0TWM2OD1|OD65OFMyKM7:TR?= NVLUdXB5W0GQR1XS
PAN1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDyeHNKSzVyPUO4Mlk6OTlizszN M2G4WnNCVkeHUh?=
MZ7-mel M3e5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrYTWM2OD1|OT6xNVk6KM7:TR?= MWnTRW5ITVJ?
COLO-679 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTN7Lkm3NFgh|ryP MoO3V2FPT0WU
SW872 Mk\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\U[nR[UUN3ME20NE4zODNzIN88US=> M3n3THNCVkeHUh?=
HT-1197 Mmj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTRyLkK4Olkh|ryP NV73NJRNW0GQR1XS
ES6 MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHtTWM2OD12MD60OVUzKM7:TR?= M{\WOHNCVkeHUh?=
SNU-387 M1P0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzKfm5kUUN3ME20NE45OjN6IN88US=> MoDSV2FPT0WU
T47D M{Lo[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTRzLkCxPVIh|ryP NW\UR5pvW0GQR1XS
G-402 NHrOOo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIn2[HpKSzVyPUSxMlA5ODlizszN MmL5V2FPT0WU
MZ1-PC NY\GfmJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIO3cZVKSzVyPUSxMlgyKM7:TR?= NIrz[ndUSU6JRWK=
SW1417 M3Xq[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\ZTGlEPTB;NEKuN|A{KM7:TR?= MVTTRW5ITVJ?
RERF-LC-MS NEH5Z5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjaU21sUUN3ME20Nk42ODh5IN88US=> MYnTRW5ITVJ?
SF539 M1vqemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn72TWM2OD12Mj61OVI6KM7:TR?= NYDYXodxW0GQR1XS
ESS-1 M2PTSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4np[GlEPTB;NEOuOVU2QCEQvF2= M1npPHNCVkeHUh?=
RO82-W-1 NVvEdHB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XqO2lEPTB;NEOuOlE2OyEQvF2= MkHaV2FPT0WU
S-117 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTR|Lk[5OVgh|ryP MnPpV2FPT0WU
SW756 NEiyZ3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnp[4RKUUN3ME20N{45OjR{IN88US=> Mkf1V2FPT0WU
CP66-MEL Mkj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUSwVVVqUUN3ME20OU44OTR|IN88US=> M3vQe3NCVkeHUh?=
H-EMC-SS NWTVeopjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTR3Lke2PVMh|ryP MonjV2FPT0WU
NCI-H2052 Mn3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHpTItFUUN3ME20OU46ODJ5IN88US=> MYDTRW5ITVJ?
SW684 MmjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fFeGlEPTB;NEeuNFA5OSEQvF2= MWLTRW5ITVJ?
HCC1569 NWLDcpg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTR5LkG2OVgh|ryP MU\TRW5ITVJ?
KGN NYXsOVlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUixTINwUUN3ME20O{4{OzFzIN88US=> NH;5WXJUSU6JRWK=
LCLC-103H MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2THSWlEPTB;NEeuOFQxPCEQvF2= M3PLcnNCVkeHUh?=
SW780 NF\KRVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTR5Lk[zOVEh|ryP M{HtUHNCVkeHUh?=
NCI-H1703 M{\FfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR6LkOzOVIh|ryP M162ZXNCVkeHUh?=
HCC1395 NIHmb2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTR6Lke0N|Ih|ryP NF;KT|dUSU6JRWK=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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 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):
1% CMC Na
混合させたのち直ちに使用することを推奨します。
30mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程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
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03720873 Recruiting EGFR Gene Mutation Fujian Cancer Hospital October 2018 Phase 2
NCT03599518 Recruiting Non Small Cell Lung Cancer Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. October 10 2018 Phase 1
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
NCT03602027 Not yet recruiting Non-squamous Non-small Cell Lung Cancer Second Affiliated Hospital of Nanchang University August 1 2018 Not Applicable
NCT03656393 Recruiting NSCLC|EGFR Shenzhen People''s Hospital August 31 2018 Phase 3
NCT03529084 Withdrawn Carcinoma Non-small Cell Lung Novartis Pharmaceuticals|Novartis July 23 2018 Phase 3

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

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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.

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