Larotinib

Modify Date: 2024-01-22 15:38:24

Larotinib Structure
Larotinib structure
Common Name Larotinib
CAS Number 1438072-11-7 Molecular Weight 488.94
Density N/A Boiling Point N/A
Molecular Formula C24H26ClFN4O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Larotinib


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].

 Names

Name Larotinib

 Larotinib Biological Activity

Description 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].
Related Catalog
Target

EGFRL861Q:0.423 nM (IC50)

EGFRL858R:0.563 nM (IC50)

EGFR (WT):0.611 nM (IC50)

EGFRT790M:45.2 nM (IC50)

HER4:84 nM (IC50)

BLK:102 nM (IC50)

IRAK1:167 nM (IC50)

BTK:196 nM (IC50)

HER2:253 nM (IC50)

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]。
References

[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.  

 Chemical & Physical Properties

Molecular Formula C24H26ClFN4O4
Molecular Weight 488.94
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.