Larotinib mesylate hydrate

Modify Date: 2025-08-25 10:36:50

Larotinib mesylate hydrate Structure
Larotinib mesylate hydrate structure
Common Name Larotinib mesylate hydrate
CAS Number 2097129-93-4 Molecular Weight 699.17
Density N/A Boiling Point N/A
Molecular Formula C26H36ClFN4O11S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Larotinib mesylate hydrate


Larotinib mesylate hydrate 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 mesylate hydrate

 Larotinib mesylate hydrate Biological Activity

Description Larotinib mesylate hydrate 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)

IRAK-1:167 nM (IC50)

BTK:196 nM (IC50)

HER2:253 nM (IC50)

In Vivo 每日给 Larotinib mesylate hydrate 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 hydrate 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 C26H36ClFN4O11S2
Molecular Weight 699.17
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