| CAS NO: | 1214265-57-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 481.01 |
|---|---|
| Formula | C24H25ClN6OS |
| CAS No. | 1214265-57-2 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 96 mg/mL (199.6 mM) |
| Water: <1 mg/mL | |
| Ethanol: 3 mg/mL (6.2 mM) | |
| Other info | Chemical Name: N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylamide InChi Key: KIISCIGBPUVZBF-UHFFFAOYSA-N InChi Code: InChI=1S/C24H25ClN6OS/c1-3-22(32)27-18-5-4-6-20(15-18)33-23-21(25)16-26-24(29-23)28-17-7-9-19(10-8-17)31-13-11-30(2)12-14-31/h3-10,15-16H,1,11-14H2,2H3,(H,27,32)(H,26,28,29) SMILES Code: C=CC(NC1=CC=CC(SC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1)=O |
| Synonyms | WZ8040; WZ 8040; WZ8040; |
| In Vitro | In vitro activity: 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. Cell Assay: Cells (HCC827, H3255, HCC827 GR, H1975, PC9, PC9 GR, Calu-3, H1819, and Ba/F3) are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay. |
|---|---|
| In Vivo | WZ4002 inhibits EGFR phosphorylation and induces significant tumor regression in murine models of EGFR T790M. |
| Animal model | Murine models of EGFR T790M |
| Formulation & Dosage | |
| References | Nature. 2009 Dec 24;462(7276):1070-4. |
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