WZ-3146
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MedKoo CAT#: 406575

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.

Chemical Structure

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WZ-3146
CAS# 1214265-56-1
Instruction

Theoretical Analysis

MedKoo Cat#: 406575
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

Price and Availability

Size Price Availability Quantity
25mg USD 300 2 Weeks
50mg USD 550 2 Weeks
100mg USD 950 2 Weeks
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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:         

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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:

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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.