Cat. No.: HY-153110A

Larotinib mesylate hydrate

Customer Review

Based on 1 Customer Validation

Larotinib mesylate hydrate 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.

For research use only. We do not sell to patients.

Purity: 98.66%
CAS No.: 2097129-93-4
Formula: C₂₆H₃₆ClFN₄O₁₁S₂
Molecular Weight:699.17

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Larotinib mesylate hydrate Chemical Structure

CAS No.: 2097129-93-4

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Larotinib mesylate hydrate 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].

IC₅₀ & Target^[1]

EGFR^L861Q

0.423 nM (IC₅₀)

EGFR^L858R

0.563 nM (IC₅₀)

EGFR (WT)

0.611 nM (IC₅₀)

EGFR^T790M

45.2 nM (IC₅₀)

HER4

84 nM (IC₅₀)

BLK

102 nM (IC₅₀)

IRAK-1

167 nM (IC₅₀)

BTK

196 nM (IC₅₀)

HER2

253 nM (IC₅₀)

All EGFR Isoforms :

All IRAK Isoforms :

In Vivo

After daily administration of Larotinib mesylate hydrate, 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 hydrate 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2097129-93-4
Appearance Solid
Molecular Weight 699.17
Formula C₂₆H₃₆ClFN₄O₁₁S₂
Color White to off-white
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
Shipping

Room temperature in continental US; may vary elsewhere.
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4303 mL

7.1513 mL

14.3027 mL

5 mM

0.2861 mL

1.4303 mL

2.8605 mL

10 mM

0.1430 mL

0.7151 mL

1.4303 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
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

Keywords

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Larotinib mesylate hydrate

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

All EGFR Isoforms

All IRAK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Larotinib mesylate hydrate Related Classifications

HY-153110A Related Classifications