Avitinib (maleate dihydrate)

Avitinib (Abivertinib) maleate dihydrate 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 maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects[1][2].

Product Specifications

CAS Number

[1822357-78-7]

Product Name Alternative

Abivertinib (maleate dihydrate) ; AC0010 (maleate dihydrate)

UNSPSC

12352005

Target

Apoptosis; Btk; EGFR

Related Pathways

Apoptosis; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

O=C(C=C)NC1=CC=CC(OC2=NC(NC3=CC(F)=C(N4CCN(C)CC4)C=C3)=NC5=C2C=CN5)=C1.OC(/C=C\C(O)=O)=O.O.O

Molecular Formula

C30H34FN7O8

Molecular Weight

639.63

References & Citations

[1]Xu X, 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 Nov;15 (11) :2586-2597.|[2]Yan X, et al. Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma. J Cancer Res Clin Oncol. 2018 Apr;144 (4) :697-706.