Larotinib mesylate hydrate

Names

[ CAS No. ]:
2097129-93-4

[ Name ]:
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]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Signaling Pathways >> Immunology/Inflammation >> IRAK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK

[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

Related Compounds