| Bioactivity | Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM[1]. |
| In Vivo | 每日给 Larotinib mesylate 后，SD 大鼠无不良反应水平 (NOAEL) 为 10 mg/kg, 比格犬最低不良反应水平 (LOAEL) 为 5 mg/kg。最大耐受剂量 (MTDs) 在 SD 大鼠和比格犬中分别为 20 和 25 mg/kg[1]。Larotinib mesylate 显示出剂量依赖性的抗肿瘤结果，在肿瘤小鼠模型中，18 mg/kg 肿瘤抑制率超过 60% (数据未发表)[1]。 |
| Name | Larotinib |
| CAS | 1438072-11-7 |
| Formula | C24H26ClFN4O4 |
| Molar Mass | 488.94 |
| 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]. Liu J, et al. Phase I Trial to Evaluate the Tolerance, Pharmacokinetics and Efficacy of the Broad-Spectrum ErbB Family Inhibitor Larotinib Mesylate in Patients With Advanced Solid Tumors. Front Pharmacol. 2021 Feb 18;12:636324. |
Larotinib
CAS: 1438072-11-7 F: C24H26ClFN4O4 W: 488.94
Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with
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