| CAS NO: | 1421373-66-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| Molecular Weight (MW) | 595.72 |
|---|---|
| Formula | C29H37N7O5S |
| CAS No. | 1421373-66-1 (mesylate); 1421373-65-0 (free base) |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO:> 100mg/mL |
| Water: N/A | |
| Ethanol: N/A | |
| Solubility (In vivo) | 1% DMSO+30% PEG 300+dd H2O: 30mg/mL |
| Synonyms | AZD-9291 mesylate; Mereletinib mesylate; AZD9291; AZD 9291; Trade name: Tagrisso Chemical Name: N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide mesylate InChi Key: FUKSNUHSJBTCFJ-UHFFFAOYSA-N InChi Code: InChI=1S/C28H33N7O2.CH4O3S/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24;1-5(2,3)4/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32);1H3,(H,2,3,4) SMILES Code: CN(CCN(C)C)C1=CC(OC)=C(C=C1NC(C=C)=O)NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2.OS(=O)(C)=O |
| In Vitro | In vitro activity: AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. Kinase Assay: Osimertinib (formerly known as AZD-9291 and mereletinib) is an oral available, irreversible, and mutant-selective, 3rd generation 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. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines. Cell Assay: AZD9291 potently inhibits EGFR phosphorylation in EGFRm+ (e.g. PC9; < 25 nM) and EGFR m+/T790M (e.g. H1975; < 25 nM) cell lines in vitro, whilst demonstrating much less activity against wild-type EGFR lines (e.g. LoVo;> 500 nM). Consistently, AZD9291 showed significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. |
|---|---|
| In Vivo | 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. |
| Animal model | EGFRm+ and EGFRm+/T790M transgenic mice |
| Formulation & Dosage | 5 mg/kg; p.o |
| References | Transl Lung Cancer Res. 2014 Dec;3(6):370-2; J Med Chem. 2014 Oct 23;57(20):8249-67. |
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