Nazartinib
Cat. No.：YN340115
CAS No. ：1508250-71-2
| 产品名称: | Nazartinib |
| CAS No.: | 1508250-71-2 |
| Chemical Name: | N-[7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1H-azepin-3-yl]-1H-benzimidazol-2-yl]-2-methyl-4-pyridinecarboxamide |
| Synonyms: | 那扎替尼; EGF816 |
| 分子量: | 495.02 |
| 分子式: | C₂₆H₃₁ClN₆O₂ |
| 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 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Nazartinib (EGF816) 是一种新颖的EGFR抑制剂，对 EGFR(L858R/790M) 突变体的Ki和Kinact值分别为 31 nM 和 0.222 min−1。 |
| IC50和靶点: | [{name:"EGFRL858R/T790M:31 nM (Ki)"}] |
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| Solvent & Solubility: |
Lelais, G., Epple, R., Marsilje, T.H., 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 (T790M) EGFR mutants for the treatment of EGFR mutant non-small-cell lung cancersJ. Med. Chem.59(14),6671-6689(2016)
Jia, Y., Juarez, J., Li, J., 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 receptorCancer Res.76(6),1591-1602(2016)
