Osimertinib (AZD9291)
製品コードS7297
分子量(MW)：499.61
Osimertinib (AZD9291) 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.
-PKI-587-J-Biol-Chem-20150728.gif)
カスタマーフィードバック(9)
-
(C,D) The Ba/F3 cells expressing EGFR-T854A/C797S/del19 (C) and EGFR-T854A/C797S/L858R (D) were treated with gefitinib, afatinib, osimertinib, and brigatinib for 6 hours at indicated concentrations. EGFR phosphorylation and downstream signal pathway were evaluated by Western blotting.
J Thorac Oncol, 2018, 13(7):915-925. Osimertinib (AZD9291) purchased from Selleck.
(C) Immunoblotting of lysates from EGFR L858R and EGFR L858M/L861Q NIH-3T3 cells treated with the indicated concentrations of gefitinib, osimertinib, or afatinib. The ratio of phospho-EGFR in treated vs. untreated samples was quantified by densitometry for each cell line.
J Thorac Oncol, 2017, 12(5):884-889. Osimertinib (AZD9291) purchased from Selleck.
-
Protein expression detected by Western blotting in PC-9 cells (left), PC-3 cells (middle), and PC-9BIMi2−/− cells (right), incubated with gefitinib (1 μmol/L), afatinib (1 μmol/L), or osimertinib (1 μmol/L), for 24 hours.
Clin Cancer Res, 2017, 23(12):3139-3149. Osimertinib (AZD9291) purchased from Selleck.
Apoptosis susceptibility of H1975 and H1975-OR NSCLC cell lines following treatment with NGI-1 (10μM), Osimertinib (1μM) or a combination of both for 48 h measured with Annexin- V and 7-AAD flow cytometry as in Fig. 1. The data represents the mean ± s.d., n = 3. *P < 0.01.
Cancer Res, 2018, doi:10.1158/0008-5472.CAN-18-0505. Osimertinib (AZD9291) purchased from Selleck.
-
Lysates from MGH121 parental cells treated with 1 μM of the indicated TKIs except for AZD9291 (160 nM) for 6 hours were probed with the indicated antibodies.
Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560 . Osimertinib (AZD9291) purchased from Selleck.
Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells.
Cancer Res, 2017, 77(8):2078-2089. Osimertinib (AZD9291) purchased from Selleck.
-
F, PC-9/ffluc and PC-9/LMC-GR cells (2×103 cells/well) were incubated with various concentrations of osimertinib for 72 hours. Cell viability was determined by MTT assay. Bars represent SD of quadruplicate cultures. Data shown are representative of three independent experiments with similar results.
Mol Cancer Ther, 2017, 16(3):506-515. Osimertinib (AZD9291) purchased from Selleck.
Western blot analysis showing phospho-EGFR (p-EGFR), total EGFR, phospho-ERK (p-ERK), total ERK, phospho-AKT (p-AKT), total AKT and β-actin as a loading control in H1975 cells treated with the indicated inhibitors. Equivalent amounts of proteins from whole cell lysates were subjected to WB analysis to detect the indicated proteins.
J Biol Chem, 2015, 290(28): 17495-504. Osimertinib (AZD9291) purchased from Selleck.
-
J Cancer Res Clin Oncol, 2018, doi:10.1007/s00432-018-2668-7. Osimertinib (AZD9291) 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 | Osimertinib (AZD9291) 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 |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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 |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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： |
+ 展開
|
|---|
溶解度 (25°C)
| 体外 | DMSO | 99 mg/mL (198.15 mM) warming |
|---|---|---|
| Ethanol | 43 mg/mL warmed (86.06 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% DMSO+30% PEG 300+ddH2O 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 | 499.61 |
|---|---|
| 化学式 | C28 H33 N7 O2 |
| CAS No. | 1421373-65-0 |
| 保管 | 粉 |
| in solvent | |
| 別名 | N/A |
便利ツール
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
*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
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 )
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。
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：
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
臨床試験
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03257124 | Recruiting | Non-Small Cell Lung Cancer With EGFR T790M Mutation|With Brain and/or Leptomeningeal Metastasis|Failed Tyrosine Kinase Inhibitors | Samsung Medical Center | May 8 2017 | Phase 2 |
| NCT02923947 | Recruiting | Solid Tumours | AstraZeneca|Quintiles Inc. | May 4 2017 | Phase 1 |
| NCT02811354 | Recruiting | Carcinoma Non-Small-Cell Lung | National University Hospital Singapore|AstraZeneca|Singapore Clinical Research Institute | February 24 2017 | Phase 2 |
| NCT02972333 | Not yet recruiting | EGFR-TKI Resistant Mutation|Nonsmall Cell Lung Cancer|AZD9291|Brain Metastases | Shandong Cancer Hospital and Institute|AstraZeneca | December 2016 | Phase 3 |
| NCT02997501 | Active not recruiting | Lung Cancer | AstraZeneca|TigerMed | December 23 2016 | Phase 3 |
| NCT02771314 | Recruiting | Non Small Cell Lung Cancer | Hellenic Oncology Research Group | June 2016 | Phase 2 |
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。
他に質問がある場合は、お気軽にお問い合わせください。
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.
