Avitinib maleate dihydrate  (Synonyms: Abivertinib maleate dihydrate; AC0010 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].

Avitinib maleate dihydrate (AC0010; 0.13 nM-2 μM; 2 h) 选择性抑制 NCI-H1975 和 NIH/3T3_TC32T8 细胞中突变型 EGFR 磷酸化，IC₅₀ 值分别为 7.3 和 2.8 nM，比抑制作用敏感约 115 倍和 298 倍 A431 中的野生型 EGFR。Avitinib maleate dihydrate 有效抑制 NCI-H1975 细胞中 EGFR-Tyr1068 磷酸化，NCI-H1975 细胞的选择性比是 A431 细胞的 65 倍。除了抑制 EGFR-Tyr1068 磷酸化外，Avitinib maleate dihydrate 还抑制 NCI-H1975 和 HCC827 细胞中下游靶标 Akt 和 ERK1/2 的磷酸化^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Avitinib maleate dihydrate (AC0010；12.5-500 mg/kg；口服；每日一次；持续 14 天) 在异种移植模型中长期抑制 EGFR 突变型肿瘤生长，但不抑制野生型 EGFR 肿瘤生长^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

639.63

C₃₀H₃₄FN₇O₈

1822357-78-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]