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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

🥰Excellent

Purity: 98.45%

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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Expected start date of shipmentUSA 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:98.45%

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COA HPLC 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	EGFR (WT):0.611 nM, HER4:84 nM, EGFR (T790M):45.2 nM, BLK:102 nM, IRAK1:167 nM, EGFR (L861Q):0.423 nM, BTK:196 nM, HER2:253 nM, EGFR (L858R):0.563 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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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