ZW-49
ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer.
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- CAS No.: 2055109-19-6
- 화학식: C33H32N8O3
- 분자량:588.66
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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All EGFR Isoforms
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Biological Activity
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HER2 |
ZW-49 potently inhibits a broad panel of mutant EGFR kinases, including EGFRL858R/T790M with an IC50 of 1.5 nM, and shows 6.6-fold selectivity over wild-type EGFR (IC50 = 9.9 nM), while also targeting select HER2 mutants[1].
ZW-49 (72 h) potently inhibits proliferation of EGFR-mutant cell lines, including NCI-H1975 (IC50 = 12 nM) and HCC827 (IC50 = 4 nM), as well as Ba/F3 cells with non-classical EGFR mutations (IC50 = 0.58-5.59 nM), while also inhibits HER2-overexpressing cells[1].
ZW-49 (1-1000 nM; 2 h) potently and dose-dependently inhibits EGFR phosphorylation and downstream AKT/ERK signaling in EGFR-mutant cell lines, including NCI-H1975, HCC827, and Ba/F3 cells expressing non-classical mutations[1].
ZW-49 (0.01-1 μM) induces G0/G1 phase cell-cycle arrest and apoptosis in H1975 cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cancer cell lines (NCI-H1975, HCC827, Ba/F3 with EGFR G719A and D770-N771insNPG, A431)
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:2 h
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Result:Completely abrogated phosphorylation of EGFR, AKT, and ERK in NCI-H1975 and HCC827 cells at 10 nM.
Exerted dose-dependent inhibition of p-EGFR, p-AKT, and p-ERK at concentrations from 1 to 1000 nM in Ba/F3 cells expressing EGFR G719A and D770-N771insNPG, while total protein levels remained stable.
Inhibited EGFR phosphorylation and downstream signaling in A431 cells at 100 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (nu/nu) mice (4–6 weeks old) xenograft models bearing H1975, BaF3-EGFR D770-N771insNPG, BaF3-EGFR G719A, or A431 cell lines[1]
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Dosage:p.o.; qd; 2 weeks
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Administration:p.o.; qd; 2 weeks
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Result:Reduced tumor volume.
Showed no significant weight change and obvious pathological changes.
Reduced phosphorylated EGFR levels and p-AKT and p-ERK levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2055109-19-6
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분자량 588.66
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화학식 C33H32N8O3
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SMILES
C=CC(NC1=CC(N2C(C(C3=CC=CC=C3)=NC4=C2N=C(N=C4)NC5=CC=C(C=C5OC)N6CCN(CC6)C)=O)=CC=C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZW-49 Related Classifications
HY-181954 Related Classifications
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