Cat. No.: HY-153110

Larotinib

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Based on 1 Customer Validation

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.

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

Purity: 99.50%
CAS No.: 1438072-11-7
Formula: C₂₄H₂₆ClFN₄O₄
Molecular Weight:488.94

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Larotinib Chemical Structure

CAS No.: 1438072-11-7

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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
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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].

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)

IRAK1

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, 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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1438072-11-7
Appearance Solid
Molecular Weight 488.94
Formula C₂₄H₂₆ClFN₄O₄
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
Shipping

Room temperature in continental US; may vary elsewhere.

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)

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

2.0452 mL

10.2262 mL

20.4524 mL

5 mM

0.4090 mL

2.0452 mL

4.0905 mL

10 mM

0.2045 mL

1.0226 mL

2.0452 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. 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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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
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

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

Keywords

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Larotinib

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical 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

Clinical Compound Library Plus

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 Related Classifications

HY-153110 Related Classifications