Avitinib (maleate)

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

Product Specifications

CAS Number

[1557268-88-8]

Product Name Alternative

Abivertinib (maleate) ; AC0010 (maleate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Btk; EGFR

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Avitinib_maleate.html

Purity

99.86

Solubility

DMSO : ≥ 100 mg/mL|H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C30H30FN7O6

Molecular Weight

603.60

Precautions

H302, H315, H319, H335

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;144 (4) :697-706.