product name WZ8040
Description: WZ8040 is a novel and potent mutant-selective irreversible EGFRT790M inhibitor with potential anticancer activity, it does not inhibit ERBB2 phosphorylation (T798I). WZ8040 is about 30-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than other quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ-8040 may be clinically more effective and better tolerated than quinazoline-based inhibitors.
References: Nature. 2009 Dec 24;462(7276):1070-4.
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)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19417036
| 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. Kinase Assay: 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. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Nature. 2009 Dec 24;462(7276):1070-4. |
Integrin Antagonist 2 (hydrochloride)
