Larotinib mesylate hydrate
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 98.66%
- CAS No.: 2097129-93-4
- Formula: C26H36ClFN4O11S2
- Molecular Weight:699.17
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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 mesylate hydrate (100 μM) inhibits PRDX1 Tyr194 phosphorylation in HRECs at a minimum effective dose of 100 μM[2].
Larotinib mesylate hydrate (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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2097129-93-4
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Appearance Solid
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Molecular Weight 699.17
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Formula C26H36ClFN4O11S2
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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.CS(=O)(O)=O.CS(=O)(O)=O.O
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Synonyms
Z650 mesylate hydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (35.76 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (285 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 1.4303 mL | 7.1513 mL | 14.3027 mL | 35.7567 mL |
| 5 mM | 0.2861 mL | 1.4303 mL | 2.8605 mL | 7.1513 mL | |
| 10 mM | 0.1430 mL | 0.7151 mL | 1.4303 mL | 3.5757 mL | |
| 15 mM | 0.0954 mL | 0.4768 mL | 0.9535 mL | 2.3838 mL | |
| 20 mM | 0.0715 mL | 0.3576 mL | 0.7151 mL | 1.7878 mL | |
| 25 mM | 0.0572 mL | 0.2861 mL | 0.5721 mL | 1.4303 mL | |
| 30 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1919 mL |
Larotinib mesylate hydrate Related Classifications
HY-153110A Related Classifications
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Keywords
- Larotinib mesylate
- 2097129-93-4
- Z650 mesylate
- EGFR
- IRAK
- Btk
- RIP kinase
- Epidermal growth factor receptor
- ErbB-1
- HER1
- Interleukin-1 receptor associated kinase
- IL-1R associated kinase
- Bruton tyrosine kinase
- Receptor-interacting protein kinases
- RIPK
- BLK
- BTK
- ErbB family receptor tyrosine kinase
- HER2
- HER4
- IRAK1
- PRDX1
- RIPK2
- advanced solid tumors
- Inhibitor
- inhibitor
- inhibit