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Larotinib

Name: Larotinib
Brand: TargetMol
SKU: T73334
Price: 74 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T73334Cas No. 1438072-11-7

Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.

Larotinib

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Purity: 99.73%

Catalog No. T73334Cas No. 1438072-11-7

Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$74	In Stock	In Stock
5 mg	$179	In Stock	In Stock
10 mg	$272	In Stock	In Stock
25 mg	$463	In Stock	In Stock
50 mg	$662	In Stock	In Stock
100 mg	$928	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.73%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.
Targets&IC50	HER4:84 nM, HER2:253 nM, EGFR (L858R):0.563 nM, EGFR (L861Q):0.423 nM, EGFR (T790M):45.2 nM, BTK:196 nM, BLK:102 nM, EGFR (WT):0.611 nM, IRAK1:167 nM
In vivo	Larotinib (250, 300, 350 mg; oral; once daily; patients) demonstrated promising antitumor activity and manageable safety profiles in patients with pre-treated advanced ESCC with EGFR overexpression or amplification, especially at the dose of 350 mg, which showed better efficacy and acceptable safety. A phase 3 study is underway on 350 mg larotinib in ESCC patients with EGFR overexpression.[1]

Chemical Properties

Molecular Weight	488.94
Formula	C₂₄H₂₆ClFN₄O₄
Cas No.	1438072-11-7
Smiles	N(C=1C2=C(C=C(OC)C(OCCCN3C[C@@]4([C@](C3)(OCCO4)[H])[H])=C2)N=CN1)C5=CC(Cl)=C(F)C=C5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (122.71 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0452 mL	10.2262 mL	20.4524 mL	102.2620 mL
5 mM	0.4090 mL	2.0452 mL	4.0905 mL	20.4524 mL
10 mM	0.2045 mL	1.0226 mL	2.0452 mL	10.2262 mL
20 mM	0.1023 mL	0.5113 mL	1.0226 mL	5.1131 mL
50 mM	0.0409 mL	0.2045 mL	0.4090 mL	2.0452 mL
100 mM	0.0205 mL	0.1023 mL	0.2045 mL	1.0226 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc