| Bioactivity | 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]. |
| Invitro | 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. 0 --> Avitinib maleate dihydrate 相关抗体: |
| In Vivo | 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. |
| CAS | 1822357-78-7 |
| Formula | C30H34FN7O8 |
| Molar Mass | 639.63 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
Avitinib maleate dihydrate
CAS: 1822357-78-7 F: C30H34FN7O8 W: 639.63
Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor,
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