2097129-93-4
Chemical Structure
Larotinib mesylate hydrate
Synonym(s): Z650 mesylate hydrate
- CAS No.: 2097129-93-4
- Formula:C26H36ClFN4O11S2
- Molecular Weight:699.17
IUPAC Name: N-(3-chloro-4-fluorophenyl)-6-(3-((4aR,7aS)-hexahydro-6H-[1,4]dioxino[2,3-c]pyrrol-6-yl)propoxy)-7-methoxyquinazolin-4-amine dimethanesulfonate hydrate
InChIKey: SOZDTNWXBLYRLP-GQOINVLUSA-N
SMILES: COC(C(OCCCN1C[C@]2([H])[C@](OCCO2)([H])C1)=C3)=CC4=C3C(NC5=CC(Cl)=C(C=C5)F)=NC=N4.CS(=O)(O)=O.CS(=O)(O)=O.O
Biological Activity: Larotinib (Z650) mesylate hydrate is an orally active ErbB family receptor tyrosine kinase inhibitor with EGFR as its primary target and an IC50 of 0.6 nM. Larotinib mesylate hydrate inhibits wild-type and mutant EGFR as well as HER2/HER4 (IC50 of 253 and 84 nM). Larotinib mesylate hydrate inhibits RIPK2, IRAK1, BTK, and BLK, with target IC50 values of 26.6, 167, 196, and 102 nM, respectively. Larotinib mesylate hydrate is primarily metabolized by CYP3A4 in vitro. Larotinib mesylate hydrate can be used for research on advanced solid tumors[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Larotinib mesylate hydrate | 98.66% | Larotinib (Z650) mesylate hydrate is an orally active ErbB family receptor tyrosine kinase inhibitor with EGFR as its primary target and an IC50 of 0.6 nM. Larotinib mesylate hydrate inhibits wild-type and mutant EGFR as well as HER2/HER4 (IC50 of 253 and 84 nM). Larotinib mesylate hydrate inhibits RIPK2, IRAK1, BTK, and BLK, with target IC50 values of 26.6, 167, 196, and 102 nM, respectively. Larotinib mesylate hydrate is primarily metabolized by CYP3A4 in vitro. Larotinib mesylate hydrate can be used for research on advanced solid tumors. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
-
Similarity Score 0.89
HY-153110Larotinib -
Similarity Score 0.73
HY-50895Gefitinib -
Similarity Score 0.73
HY-50895AGefitinib hydrochloride -
Similarity Score 0.73
HY-50895BGefitinib dihydrochloride -
Similarity Score 0.70
HY-W109039EGFR ligand-15 -
Similarity Score 0.69
HY-100636Gefitinib N-oxide -
Similarity Score 0.68
HY-168305EGFR ligand-11 -
Similarity Score 0.67
HY-W561311M387783 -
Similarity Score 0.67
HY-153111EGFR/HER2-IN-9 -
Explore the MedChemAI to find more analogs
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. [Content Brief]
- [2]. Yang M, et al. KIF11 prevents retinal endothelial ferroptosis in familial exudative vitreoretinopathy by inhibiting phosphorylation-driven PRDX1 phase separation. Nature communications. 2026 Mar 24;17(1):4360. [Content Brief]
