Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible, orally active, selective EGFR inhibitor with IC50 values of 0.18 nM, 0.18 nM, and 7.68 nM for EGFR L858R, EGFR T790M, and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis in mantle cell lymphoma cells and inhibits BTK phosphorylation. Avitinib maleate dihydrate exhibits anticancer effects.

Physicochemical Properties

Molecular Formula	C30H34FN7O8
Molecular Weight	639.63
CAS #	1822357-78-7
Related CAS #	Avitinib;1557267-42-1;Avitinib maleate;1557268-88-8
SMILES	FC1C=C(C=CC=1N1CCN(C)CC1)NC1N=C(C2C=CNC=2N=1)OC1C=CC=C(C=1)NC(C=C)=O.OC(/C=C\C(=O)O)=O.O.O
Synonyms	Abivertinib maleate dihydrate; AC0010 maleate dihydrate
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Avitinib maleate dihydrate (AC0010; 0.13 nM-2 μM; 2 h) selectively inhibits mutant EGFR phosphorylation in NCI-H1975 and NIH/3T3_TC32T8 cells with IC50 values of 7.3 and 2.8 nM, respectively, which are approximately 115-fold and 298-fold more sensitive than the inhibition of wild-type EGFR in A431. Avitinib maleate dihydrate potently inhibits EGFR-Tyr1068 phosphorylation in NCI-H1975 cells with a 65-fold selectivity for NCI-H1975 cells over A431 cells. In addition to inhibiting EGFR-Tyr1068 phosphorylation, Avitinib maleate dihydrate also inhibits phosphorylation of downstream targets Akt and ERK1/2 in NCI-H1975 and HCC827 cells [1].
ln Vivo	Avitinib maleate dihydrate (AC0010; 12.5-500 mg/kg; oral; once daily; for 14 days) has long-term inhibition of EGFR mutant tumor growth in xenograft models, but not wild-type EGFR tumor growth [1].
References	[1]. 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]. Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma. J Cancer Res Clin Oncol. 2018 Apr;144(4):697-706.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.5634 mL	7.8170 mL	15.6340 mL
	5 mM	0.3127 mL	1.5634 mL	3.1268 mL
	10 mM	0.1563 mL	0.7817 mL	1.5634 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.