WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406575
CAS#: 1214265-56-1
Description: WZ-3146 is a covalent or irreversible pyrimidine-based EGFR inhibitor against EGFR T790M. WZ-3146 was identified by screening an irreversible kinase inhibitor library specifically against EGFR T790M. WZ-3146 potently suppresses the growth of EGFR-T790M-containing cell lines and inhibits EGFR phosphorylation. WZ-3146 is also effective in murine models of lung cancer driven by EGFR T790M. WZ-3146 may be clinically more effective and better tolerated than quinazoline-based inhibitors. All current EGFR inhibitors possess a structurally related quinazoline-based core scaffold and were identified as ATP-competitive inhibitors of wild-type EGFR.
Hodoodo Cat#: H406575
Name: WZ-3146
CAS#: 1214265-56-1
Chemical Formula: C24H25ClN6O2
Exact Mass: 464.17
Molecular Weight: 464.950
Elemental Analysis: C, 62.00; H, 5.42; Cl, 7.63; N, 18.08; O, 6.88
Synonym: WZ3146; WZ-3146; WZ 3146.
IUPAC/Chemical Name: N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)acrylamide
InChi Key: APHGZZPEOCCYNO-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H25ClN6O2/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(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1)=O
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).
HS Tariff Code: 2934.99.9001
More Info:
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The following data is based on the product molecular weight 464.95 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
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.