WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor with potential anticancer activity. 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.

MedKoo Cat#: 406574 Name: WZ-8040 CAS#: 1214265-57-2 Chemical Formula: C24H25ClN6OS Exact Mass: 480.14991 Molecular Weight: 481.01 Elemental Analysis: C, 59.93; H, 5.24; Cl, 7.37; N, 17.47; O, 3.33; S, 6.67

Synonym: WZ8040; WZ8040; WZ 8040.

IUPAC/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/h4-10,15-16H,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

Technical Data

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

        

References

1: Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622. PubMed PMID: 20033049; PubMed Central PMCID: PMC2879581.

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