Avitinib dihydrochloride
Based on 1 publication(s) in Google Scholar
Avitinib (Abivertinib) dihydrochloride is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib dihydrochloride is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib dihydrochloride shows anticancer effects.
For research use only. We do not sell to patients.
- CAS No.: 1557268-90-2
- Formula: C26H28Cl2FN7O2
- Molecular Weight:560.45
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Avitinib dihydrochloride
MoreAll EGFR Isoforms
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Biological Activity
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EGFR L858R 0.18 nM (IC50) |
EGFRT790M 0.18 nM (IC50) |
EGFR (WT) 7.68 nM (IC50) |
Avitinib (AC0010; 0.13 nM-2 μM; 2 h) dihydrochloride selectively inhibits mutant EGFR phosphorylation with IC50 values of 7.3 and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells, about 115- and 298-fold more sensitive than that of the inhibition of wild-type EGFR in A431. Avitinib dihydrochloride potently inhibits EGFR-Tyr1068 phosphorylation in NCI-H1975 cells, and the selectivity ratio is at 65-fold for NCI-H1975 cells versus A431 cells. In addition to inhibition of EGFR-Tyr1068 phosphorylation, Avitinib dihydrochloride inhibits phosphorylation of the downstream targets Akt and ERK1/2 in NCI-H1975 and HCC827 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H1975, HCC827, A431 cells
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Concentration:0.13 nM, 0.64 nM, 3.2 nM, 16 nM, 80 nM, 0.4 μM, 2 μM
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Incubation Time:2 h
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Result:Selectively inhibits mutant EGFR phosphorylation with IC50 values of 7.3 and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nu/Nu nude mice (Six- to 8-week-old) injected with NCI-H1975 and A431 cells[1]
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Dosage:12.5, 50, and 500 mg/kg
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Administration:Orally administration; once daily; for 14 days
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Result:Inhibited EGFR-mutant tumor growth but not wild-type EGFR tumor growth.
Chemical Information
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CAS No. 1557268-90-2
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Molecular Weight 560.45
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Formula C26H28Cl2FN7O2
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SMILES
O=C(NC1=CC(OC2=NC(NC3=CC=C(N4CCN(CC4)C)C(F)=C3)=NC5=C2C=CN5)=CC=C1)C=C.Cl.Cl
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Synonyms
Abivertinib dihydrochloride; AC0010 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Antioxidants (Basel)
A Novel SIRT1 Activator Hydroxygenkwanin Alleviates Osteoporosis by Inhibiting Ferroptosis and Lactylation in Skeletal Stem/Progenitor Cells. [Abstract]2026 May 12;15(5):612. PMID: 42193234
Purity & Documentation
References
[1]. Xu X, Mao L, Xu W, et al. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther. 2016;15(11):2586-2597. [Content Brief]
[2]. Yan X, Zhou Y, Huang S, et al. Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma. J Cancer Res Clin Oncol. 2018;144(4):697-706. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Avitinib dihydrochloride Related Classifications
HY-183397 Related Classifications
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