Nazartinib
Based on 9 publication(s) in Google Scholar
Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.53%
- CAS 番号: 1508250-71-2
- 分子式: C26H31ClN6O2
- 分子量:495.02
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Nazartinib
More- Cancer Res. 2021 Sep 15;81(18):4822-4834. [Abstract]
- Cancer Lett. 2021 Oct 28:519:141-149. [Abstract]
- R Soc Open Sci. 2020 Jan 15;7(1):191595. [Abstract]
- R Soc Open Sci. 2019 Aug 14;6(8):190852. [Abstract]
- Patent. US20250312348A1.
- Patent. US20220177473A1.
- Patent. US20220175778A1.
- Patent. US20210361655A1.
- Patent. US20190160066A1
EGFR アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
EGFRL858R/T790M 31 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HaCaT | IC50 |
160.6 nM
Compound: 47; EGF816
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Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method
Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method
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[PMID: 27433829] |
| NCI-H1975 | IC50 |
25 nM
Compound: EGF816
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Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as suppression of cell proliferation
Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as suppression of cell proliferation
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[PMID: 26968253] |
体外実験
Nazartinib (EGF816) has inhibitory effect on the mutant cell lines with IC50s of 4, 6, 2 nM in H1975, H3255, and HCC827, respectively, and demonstrates improved ADME and PK properties[1]. Nazartinib (EGF816) shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines with EC50 values of 5, 1, and 3 nM, respectively. Nazartinib inhibits cell proliferation, with EC50 values of 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively. Nazartinib has an OC50 (compound concentration at 50% occupancy) value of 2 and 5 nM on HCC827 and H1975, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1508250-71-2
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性状 Solid
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分子量 495.02
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分子式 C26H31ClN6O2
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Color Off-white to yellow
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SMILES
O=C(C1=CC(C)=NC=C1)NC2=NC3=CC=CC(Cl)=C3N2[C@H]4CN(C(/C=C/CN(C)C)=O)CCCC4
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別名
EGF816
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cancer Res
Targeting c-Myc to Overcome Acquired Resistance of EGFR Mutant NSCLC Cells to the Third-Generation EGFR Tyrosine Kinase Inhibitor, Osimertinib. [Abstract]2021 Sep 15;81(18):4822-4834. PMID: 34289988 -
Cancer Lett
Inhibition of MEK5/ERK5 signaling overcomes acquired resistance to the third generation EGFR inhibitor, osimertinib, via enhancing Bim-dependent apoptosis. [Abstract]2021 Oct 28:519:141-149. PMID: 34245854 -
R Soc Open Sci
Spectroscopic and molecular docking studies reveal binding characteristics of nazartinib (EGF816) to human serum albumin. [Abstract]2020 Jan 15;7(1):191595. PMID: 32218978 -
R Soc Open Sci
Liquid chromatography-tandem mass spectrometry metabolic profiling of nazartinib reveals the formation of unexpected reactive metabolites. [Abstract]2019 Aug 14;6(8):190852. PMID: 31598253 -
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溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (202.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
参考文献
[1]. Lelais G, et al. Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T79 [Content Brief]
[2]. Jia Y, et al. EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor. Cancer Res. 2016 Mar 15;76(6):1591-602 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0201 mL | 10.1006 mL | 20.2012 mL | 50.5030 mL |
| 5 mM | 0.4040 mL | 2.0201 mL | 4.0402 mL | 10.1006 mL | |
| 10 mM | 0.2020 mL | 1.0101 mL | 2.0201 mL | 5.0503 mL | |
| 15 mM | 0.1347 mL | 0.6734 mL | 1.3467 mL | 3.3669 mL | |
| 20 mM | 0.1010 mL | 0.5050 mL | 1.0101 mL | 2.5252 mL | |
| 25 mM | 0.0808 mL | 0.4040 mL | 0.8080 mL | 2.0201 mL | |
| 30 mM | 0.0673 mL | 0.3367 mL | 0.6734 mL | 1.6834 mL | |
| 40 mM | 0.0505 mL | 0.2525 mL | 0.5050 mL | 1.2626 mL | |
| 50 mM | 0.0404 mL | 0.2020 mL | 0.4040 mL | 1.0101 mL | |
| 60 mM | 0.0337 mL | 0.1683 mL | 0.3367 mL | 0.8417 mL | |
| 80 mM | 0.0253 mL | 0.1263 mL | 0.2525 mL | 0.6313 mL | |
| 100 mM | 0.0202 mL | 0.1010 mL | 0.2020 mL | 0.5050 mL |
Nazartinib 関連分類
HY-12872 関連分類
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