| Identification | Back Directory | [Name]
4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-6-[3-[(4aR,7aS)-hexahydro-6H-1,4-dioxino[2,3-c]pyrrol-6-yl]propoxy]-7-methoxy-, rel- | [CAS]
1438072-11-7 | [Synonyms]
Larotinib
rel-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
4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-6-[3-[(4aR,7aS)-hexahydro-6H-1,4-dioxino[2,3-c]pyrrol-6-yl]propoxy]-7-methoxy-, rel- | [Molecular Formula]
C24H26ClFN4O4 | [MOL File]
1438072-11-7.mol | [Molecular Weight]
488.94 |
| Chemical Properties | Back Directory | [Boiling point ]
628.1±55.0 °C(Predicted) | [density ]
1.346±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
8.06±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
After daily administration of Larotinib mesylate, the no observed adverse effect level (NOAEL) is 10 mg/kg in Sprague-Dawley rats and the lowest observed adverse effect level (LOAEL) is 5 mg/kg in beagle dogs. The maximal tolerable doses (MTDs) are 20 and 25 mg/kg in Sprague-Dawley rats and beagle dogs, respectively[1].
Larotinib mesylate shows dose-dependent antitumor results and a tumor-inhibiting rate exceeding 60% at 18 mg/kg in a tumor-bearing mice model (data not published)[1]. | [IC 50]
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) | [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. DOI:10.3389/fphar.2021.636324 |
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