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 No.
- 1438072-11-7
- Chemical 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-
- 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-
- CBNumber:
- CB39806080
- Molecular Formula:
- C24H26ClFN4O4
- Molecular Weight:
- 488.94
- MDL Number:
- MOL File:
- 1438072-11-7.mol
- MSDS File:
- SDS
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- price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 44444 | Larotinib ≥98% | 1438072-11-7 | 1mg | $40 | 2026-04-30 | Buy |
| Cayman Chemical | 44444 | Larotinib ≥98% | 1438072-11-7 | 5mg | $180 | 2026-04-30 | Buy |
| Cayman Chemical | 44444 | Larotinib ≥98% | 1438072-11-7 | 10mg | $320 | 2026-04-30 | Buy |
| Cayman Chemical | 44444 | Larotinib ≥98% | 1438072-11-7 | 25mg | $550 | 2026-04-30 | Buy |
| ChemScene | CS-0650981 | Larotinib 99.50% | 1438072-11-7 | 5mg | $238 | 2026-06-04 | Buy |
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- Chemical Properties, Uses, Production
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
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- Preparation Products And Raw materials
Raw materials
Preparation Products
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- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| Tianjin Kailiqi Biotechnology Co., Ltd. | 15076683720 | klq@cw-bio.com | China | 9780 | 55 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| Zhejiang Huida Biotech Co., LTD | 0571-89903022 18679456698 | zilong@hizyme.com | China | 8001 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 | psaitong@jm-bio.com | China | 27626 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 59929 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11963 | 58 |
| Beijing Boorsen Biotechnology Co., Ltd | 400-901-9800 18611424007 | cis@bioss.com.cn | China | 9185 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| Jiangsu Aikon Biopharmaceutical R&D Co.,Ltd | 025-5885952 15955137747 | sales@aikonchem.com | China | 8012 | 58 |





