Nazartinib

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Chemical Structure| 1508250-71-2 同义名 : EGF816;NVS-816
CAS号 : 1508250-71-2
货号 : A100729
分子式 : C26H31ClN6O2
纯度 : 98%
分子量 : 495.016
MDL号 : MFCD28963918
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 200 mg/mL(404.03 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1

    mutant EGFR, Ki:0.031 μM

  • mutant EGFR

    mutant EGFR, Ki:0.031 μM
描述 Nazartinib (EGF816) exhibits an inhibitory effect on mutant cell lines, with IC50 values of 4 nM for H1975, 6 nM for H3255, and 2 nM for HCC827, and shows enhanced ADME and pharmacokinetic (PK) characteristics[1]. Nazartinib (EGF816) strongly inhibits pEGFR levels in H3255, HCC827, and H1975 cell lines, showing EC50 values of 5, 1, and 3 nM, respectively. It also effectively curbs cell proliferation, with EC50 values of 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively. Furthermore, Nazartinib exhibits OC50 values of 2 and 5 nM on HCC827 and H1975, respectively[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.10mL

2.02mL

1.01mL

20.20mL

4.04mL

2.02mL
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

[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