2097129-93-4

2097129-93-4 structure

2097129-93-4 structure

Name: Larotinib mesylate hydrate
Chemical Name: Larotinib mesylate hydrate
CAS Number: 2097129-93-4
Molecular Formula: C₂₆H₃₆ClFN₄O₁₁S₂
Molecular Weight: 699.17
Catalog: Signaling Pathways Immunology/Inflammation IRAK
Create Date: 2023-04-21 10:52:22
Modify Date: 2024-01-12 16:08:20
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].

Name	Larotinib mesylate hydrate

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.

Molecular Formula	C₂₆H₃₆ClFN₄O₁₁S₂
Molecular Weight	699.17