Osimertinib (AZD9291)

For research use only. Not for use in humans.

製品コードS7297 別名:Mereletinib

Osimertinib (AZD9291)化学構造

CAS No. 1421373-65-0

Osimertinib (AZD9291, Mereletinib) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

サイズ 価格(税別)  
JPY 12000
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バルク問合せ

文献中Selleckの製品使用例(289)

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 Osimertinib (AZD9291, Mereletinib) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.
特性 Orally bioavailable mutant-selective EGFR inhibitor that has been tested in Phase III clinical trials for treatment of Non-Small Cell Lung Cancer.
ターゲット
L858R/T790M EGFR [1]
(LoVo cells)
Exon 19 deletion EGFR [1]
(LoVo cells)
WT EGFR [1]
(LoVo cells)
11.44 nM 12.92 nM 493.8 nM
体外試験

AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC-9/BRc1 NUfudFhRTnWwY4Tpc44hSXO|YYm= NX7hT4VXPTBibl2= NGTESWczPCCq NUPtXHdPTE2VTx?= MYnpcoR2[2W|IHX4dJJme3Orb36gc4YhfGinIIDyc4Fxd3C2b4TpZ{BDS0xvMjDmZY1qdHlibXXtZoVzKEKLTR?= M1XleFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEe3N|I2Lz5{NUS3O|MzPTxxYU6=
PC-9/ERc1 M3HuTGZ2dmO2aX;uJGF{e2G7 M{L2d|UxKG6P MVSyOEBp M4DCSWROW09? MV7pcoR2[2W|IHX4dJJme3Orb36gc4YhfGinIIDyc4Fxd3C2b4TpZ{BDS0xvMjDmZY1qdHlibXXtZoVzKEKLTR?= Ml7XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
VP-2 MnXHSpVv[3Srb36gRZN{[Xl? NEH3NY42OCCwTR?= NF\GcW4zPCCq MU\EUXNQ NGPucmNqdmS3Y3XzJIV5eHKnc4Ppc44hd2ZidHjlJJBzd2Gyb4D0c5Rq[yCEQ1ytNkBn[W2rbImgcYVu[mW{IFLJUS=> MljyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
PC-9/BRc1 M4n3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2P2[lUxKG6P M1:1R|ExKGR? MkfDSG1UVw>? M4DzNYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= MkSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
PC-9/ERc1 M1f1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP1fnQ2OCCwTR?= NHvaS|UyOCCm NEDP[JNFVVOR M1rOO4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= NYDCfXI6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0O|c{OjVpPkK1OFc4OzJ3PD;hQi=>
VP-2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LYUFUxKG6P M3fPPVExKGR? NV\NUXFETE2VTx?= M3nZSolvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= MnvSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N|I2RC:jPh?=
PC9 GR4 NIHUbnVHfW6ldHnvckBCe3OjeR?= MlnkNE0yOCEQvF2= NFG5THg4OiCq MnztbY5pcWKrdIRCpGVITlJicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJJNq\26jbHnu[:Kh M1vROlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUS4OlM{Lz5{NUm0PFY{OzxxYU6=
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BAF3 NHrkdY1HfW6ldHnvckBie3OjeR?= M3W1c|czKGh? NFiwdYlIUTVyIE2gNE4xODB|IN88US=> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
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HCC827 M{jhSmZ2dmO2aX;uJIF{e2G7 NITubpc{KGh? M3P1PWlEPTBiPTCwMlAxOjVizszN MoLTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd2M{O4NlkoRjJ5NEOzPFI6RC:jPh?=
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NCI-H1975 MkXlSpVv[3Srb36gZZN{[Xl? MUC3NkBp MnvIS2k2OCB;IECuNFA2KM7:TR?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
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NCI-H1975 MojsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MYK3NkBp M373XGlEPTBiPTCwMlAyODVizszN MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDdzNk[0NUc,Ojh5MU[2OFE9N2F-
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HCC827 NHrNV5BCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M4S1TVk3KGh? NVrx[ZBjTUN3MDC9JFAvODF2IN88US=> NHfvfYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi1N|U4PSd-Mki4OVM2PzV:L3G+
NCI-H1975 NVrHbmZpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M{nnRVk3KGh? Mke5SWM2OCB;IECuNFE1KM7:TR?= M3PFOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
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human hepatocytes MVLGeY5kfGmxbjDhd5NigQ>? M4Lh[WlvfHKrboPpZ{BkdGWjcnHuZ4UhcW5iaIXtZY4hcGWyYYTvZ5l1\XNiYYPz[ZN{\WRicHXyJI1qdGyrb36gZ4VtdHN? M{fXOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEK2PVk3Lz5{OESyOlk6PjxxYU6=
rat hepatocytes NVPSbpEzTnWwY4Tpc44h[XO|YYm= M{iyUWlvfHKrboPpZ{BkdGWjcnHuZ4UhcW5icnH0JIhmeGG2b3P5eIV{KGG|c3Xzd4VlKHCncjDtbYxtcW:wIHPlcIx{ NEP0bm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESyOlk6Pid-Mki0NlY6QTZ:L3G+
A549, NCI-H1975 M1TjZ2Z2dmO2aX;uJIF{e2G7 MVHT[Yxm[3Srdnn0fUBz[XSrbzDv[kBKSzVyIH\vdkBGT0Zvc4TpcZVt[XSnZDD3bYxlKHS7cHWgSWdHWiCrbjDoeY1idiCDNUS5JINmdGy|IITvJGlEPTBiZn;yJGVITlJiTEi1PHIwXDd7MF2g[I92[mynIH31eIFvfCCrbjDoeY1idiCQQ1mtTFE6PzViY3XscJM> NETPZ289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1OlIzOid-Mk[3OVYzOjJ:L3G+
A549, PC9 MmTkSpVv[3Srb36gZZN{[Xl? Mk\yV4Vt\WO2aY\peJkhemG2aX:gc4YhUUN3MDDmc5IhTUeILYP0bY12dGG2ZXSge4lt\CC2eYDlJGVITlJiaX6gbJVu[W5iQUW0PUBk\WyuczD0c{BKSzVyIH\vdkBGT0[UIHTlcIV1cW:wIH31eIFvfCCrbjDoeY1idiCSQ{mgZ4VtdHN? NXvTNVYyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OVYzOjJpPkK2O|U3OjJ{PD;hQi=>
HCC827 NIDQXXNCeG:ydH;zbZMh[XO|YYm= MkDETY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ1O4Nlch[2WubIOgbIFz[m:{aX7nJGVITlJiRUe0OkB1dyCDN{WwJIRmdGW2aX;uJI12fGGwdDDhd5Nme3OnZDDhd{Bm[XKueTDhdI9xfG:2aXOgZ4VtdHNiYYSgN{B2VSCjZoTldkAzPCCqcoOgZpkhSW6wZYjpckBXNU[LVFOvdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZzDiZZNm\CCobH;3JIN6fG:vZYTyfUApWn[kIE2gNU4{PCC2bzCxMlY4LSl? Mon2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NUOzOFAoRjJ7OEWzN|QxRC:jPh?=
NCI-H1975 NYq1bIh2TnWwY4Tpc44h[XO|YYm= NH7tNHBKdmirYnn0bY9vKG:oIFXHSnIhVDh3OGKvWFc6OE1iZH;1ZoxmKG23dHHueEBxcG:|cHjvdplt[XSrb36gbY4hTUeILYP0bY12dGG2ZXSgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGG2IEGgeI8hOTByIH7NJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTlyNkGxOEc,Ojl7ME[xNVQ9N2F-
A431 Mmj2SpVv[3Srb36gZZN{[Xl? MnLQV4Vt\WO2aY\peJkhemG2aX:sJJJifGmxIFnDOVAh\m:{IHj1cYFvKEF2M{GgZ4VtdHNib4\ldoV5eHKnc4Ppcochf2muZD30fZBmKEWJRmKgeI8hUUN3MDDmc5IhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHX4dJJme3OrbnegSWdHWiCWN{mwUU9NQDV6UjDteZRidnR? MmrIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{G2N|koRjJ5MUOxOlM6RC:jPh?=
PC9 NF7jXZVCdnSrdIXtc5Ih[WO2aY\peJkh[XO|YYm= MV\BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{mgZ4VtdHNiaHHyZo9zcW6pIFXHSnIh\XixbjCxPUBl\WyndHnvckBi[3SrdnH0bY5oKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDTR2lFKG2xdYPlJIF{e2W|c3XkJIF{KHS3bX;yJIdzd3e2aDDpcohq[mm2aX;uJIF1KDFyIH3nM4toN2SjeTygdI8heWRiZn;yJFch\GG7czDy[YxifGm4ZTD0c{Bkd262cn;s MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ5MUm2N{c,OjV{N{G5OlM9N2F-
A431 NXTUNmFUSW62aYT1cY9zKGGldHn2bZR6KGG|c3H5 M17jRmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0N|Eh[2WubIOgfIVvd2e{YX\0[YQhcW5iU1PJSEBud3W|ZTDhd5Nme3OnZDDhd{B1fW2xcjDndo94fGhiaX7obYJqfGmxbjDheEA2KG2pL3vnM4RigSxicH:gdYQh\m:{IEeg[IF6eyC{ZXzheIl3\SC2bzDjc451em:u NVnQeGlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyO|E6PjNpPkK1NlcyQTZ|PD;hQi=>

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

アッセイ
Methods Test Index PMID
Western blot
p-EGFR / p-AKT / p-ERK; 

PubMed: 28416483     


PC-9/BRc1 cells were treated with the indicated doses of osimertinib. Drugs were refreshed every 24 hours. Cellular lysates were probed with the indicated antibodies. Osim: osimertinib.

ABCB1; 

PubMed: 27649127     


The effect of osimertinib at 0.3 μM on the expression of ABCB1 was measured in KB-3-1 and KB-C2 cell lines for 0, 24, 48, and 72 h.

28416483 27649127
Growth inhibition assay
Cell viability; 

PubMed: 31043587     


Cells were treated with gefitinib or osimertinib for 72 h. Cell viability was measured by MTT assay. *P < 0.05, **P < 0.01, ***P < 0.005 by t-test.

31043587
Immunofluorescence
Ki67 / γH2AX / p16; 

PubMed: 29212784     


PC9ER cells were treated for 5 days with either 3×mAbs (20 μg/ml), saline (CTRL), or with a low dose of osimertinib (2.5 nM). Shown are representative images of cells fixed in paraformaldehyde and immunostained for KI67 (panel E), γH2AX (panel F), and p16 (panel G). DAPI counterstaining was used to follow nuclear localization. Scale bar, 20 μm. The box and whisker plots, where the ends of the box are the upper and lower quartiles, depict quantifications of results obtained in three independent experiments. **P ≤ 0.01, ***P ≤ 0.001, n = 4; one-way ANOVA with Tukey's test.

29212784
体内試験 AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo. [2]

お薦めの試験操作(参考用のみ)

動物試験:

[2]

- 合併
  • 動物モデル: Mice bearing PC9 and H1975 xenograft tumors
  • 投薬量: ~5 mg/kg
  • 投与方法: p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 99 mg/mL (198.15 mM) warming
Water Insoluble
Ethanol '43 mg/mL warmed '43
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):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
混合させたのち直ちに使用することを推奨します。
7.5mg/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 499.61
化学式

C28 H33 N7 O2

CAS No. 1421373-65-0
Storage powder
in solvent
別名 Mereletinib
Smiles CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC

投与溶媒組成計算器(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)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
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
計算リセット

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 (mg) = 濃度 (mM) x 体積 (mL) 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SDS/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SDS/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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02841579 Completed Drug: Osimertinib Non-Small Cell Lung Cancer MedSIR|AstraZeneca August 2016 Phase 2
NCT02771314 Unknown status Drug: AZD9291 Non Small Cell Lung Cancer Hellenic Oncology Research Group August 2 2016 Phase 2
NCT02529995 Completed Drug: AZD9291 40 mg|Drug: AZD9291 80 mg Carcinoma Non-Small-Cell Lung With EGFR Mutation Positive AstraZeneca August 24 2015 Phase 1
NCT02491944 Completed Drug: AZD9291|Drug: [14C]AZD9291 Oncology AstraZeneca July 2015 Phase 1

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:

    Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?

  • 回答:

    Osimertinib can be used for animal study. The vehicle we suggest is: 1% DMSO+30% PEG 300+dd H2O at up to 30mg/ml.

EGFRシグナル伝達経路

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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