Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 9,500 | |||
5 mg | 在庫あり | ¥ 22,000 | |||
10 mg | 在庫あり | ¥ 35,500 | |||
25 mg | 在庫あり | ¥ 59,500 | |||
50 mg | 在庫あり | ¥ 88,500 | |||
100 mg | 在庫あり | ¥ 130,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 22,500 |
説明 | WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I). |
ターゲット&IC50 | Calu3 (ErbB2 amp):915 nM , H3255 (EGFR L858R):66 nM, H1975 (EGFR L858R/T790M):9 nM, HCC827 GR (EGFR E746_A750/MET amp):>3.3 μM, H1781 (ErbB2 Ins G776V, C):744 nM , PC9 (EGFR Del E746_A750):6 nM, PC9 GR (EGFR Del E746_A750/T790M):8 nM, H1819 (ErbB2 amp):738 nM , HCC827 (EGFR Del E746_A750):1 nM |
In vitro | WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells. [1] |
細胞研究 | Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.(Only for Reference) |
分子量 | 481.01 |
分子式 | C24H25ClN6OS |
CAS No. | 1214265-57-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 3 mg/mL (6.23 mM)
DMSO: 89 mg/mL (185 mM)
You can also refer to dose conversion for different animals. 詳細
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WZ8040 1214265-57-2 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER1 mutated Inhibitor phosphorylation WZ 8040 NSCLC Epidermal growth factor receptor inhibit WZ-8040 ErbB-1 inhibitor