Larotinib
Based on 1 Customer Validation
Larotinib (Z650) is an orally active ErbB family receptor tyrosine kinase inhibitor with EGFR as its primary target and an IC50 of 0.6 nM. Larotinib inhibits wild-type and mutant EGFR as well as HER2/HER4 (IC50 of 253 and 84 nM). Larotinib inhibits RIPK2, IRAK1, BTK, and BLK, with target IC50 values of 26.6, 167, 196, and 102 nM, respectively. Larotinib is primarily metabolized by CYP3A4 in vitro. Larotinib can be used for research on advanced solid tumors.
For research use only. We do not sell to patients.
- Purity : 99.50%
- CAS No.: 1438072-11-7
- Formula: C24H26ClFN4O4
- Molecular Weight:488.94
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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AEE788 (Standard)EGFR/ErbB2 Inhibitor
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
EGFRL861Q 0.423 nM (IC50) |
EGFRL858R 0.563 nM (IC50) |
EGFR (WT) 0.611 nM (IC50) |
RIPK2 26.6 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) |
In Vitro
Larotinib (100 μM) inhibits PRDX1 Tyr194 phosphorylation in HRECs at a minimum effective dose of 100 μM[2].
Larotinib (100 μM) shifts PRDX1 from high-
molecular-weight (HMW) dimers toward low-molecular-weight (LMW) monomers in KIF11-knockdown HRECs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Larotinib produces dose-dependent tumor growth inhibition in tumor-bearing mice, exceeding 60% inhibition at 18 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1438072-11-7
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Appearance Solid
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Molecular Weight 488.94
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Formula C24H26ClFN4O4
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Color White to off-white
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SMILES
COC(C(OCCCN1C[C@]2([H])[C@](OCCO2)([H])C1)=C3)=CC4=C3C(NC5=CC(Cl)=C(C=C5)F)=NC=N4
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Synonyms
Z650
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (255.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0452 mL | 10.2262 mL | 20.4524 mL | 51.1310 mL |
| 5 mM | 0.4090 mL | 2.0452 mL | 4.0905 mL | 10.2262 mL | |
| 10 mM | 0.2045 mL | 1.0226 mL | 2.0452 mL | 5.1131 mL | |
| 15 mM | 0.1363 mL | 0.6817 mL | 1.3635 mL | 3.4087 mL | |
| 20 mM | 0.1023 mL | 0.5113 mL | 1.0226 mL | 2.5566 mL | |
| 25 mM | 0.0818 mL | 0.4090 mL | 0.8181 mL | 2.0452 mL | |
| 30 mM | 0.0682 mL | 0.3409 mL | 0.6817 mL | 1.7044 mL | |
| 40 mM | 0.0511 mL | 0.2557 mL | 0.5113 mL | 1.2783 mL | |
| 50 mM | 0.0409 mL | 0.2045 mL | 0.4090 mL | 1.0226 mL | |
| 60 mM | 0.0341 mL | 0.1704 mL | 0.3409 mL | 0.8522 mL | |
| 80 mM | 0.0256 mL | 0.1278 mL | 0.2557 mL | 0.6391 mL | |
| 100 mM | 0.0205 mL | 0.1023 mL | 0.2045 mL | 0.5113 mL |
Larotinib Related Classifications
HY-153110 Related Classifications
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