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Glesatinib hydrochloride

Name: Glesatinib hydrochloride
Brand: TargetMol
SKU: T15383
Rating: 4.5 (1 reviews)

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Catalog No. T15383Cas No. 1123838-51-6

Alias MGCD265 hydrochloride

Glesatinib hydrochloride is an orally active and potent dual inhibitor of MET/SMO. Glesatinib hydrochloride is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.

Glesatinib hydrochloride

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Catalog No. T15383Alias MGCD265 hydrochlorideCas No. 1123838-51-6

Pack Size	Price	Availability
25 mg	$954	6-8 weeks
50 mg	$1,240	6-8 weeks
100 mg	$1,990	6-8 weeks

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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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Product Introduction

Bioactivity

Description	Glesatinib hydrochloride is an orally active and potent dual inhibitor of MET/SMO. Glesatinib hydrochloride is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.
In vitro	Glesatinib hydrochloride (0.01, 0.1, 0.5, 1 μM) obviously enhances by several-fold the percentage of apoptotic cells in NSCLC H1299 cells. Glesatinib hydrochloride (0.01-5 μM; for 72 hours) causes a dose-dependent inhibition of cancer cell growth (IC50: 0.08 μM on NSCLC H1299 cells). Glesatinib hydrochloride has the cytotoxicity to P-gp overexpressing cancer cells KB-C2, SW620/Ad300, HEK293/ABCB1, and their parent cells KB-3-1, SW620, HEK293 cells with the IC50s fell between 5 and 10 μM [1]. Glesatinib hydrochloride (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner. Glesatinib hydrochloride (1, 3 μM; 120 mins) enhances the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp [2].
In vivo	Glesatinib hydrochloride (15 mg/kg/day; orally; 40 weeks) results in an obvious reduction in tumor size [1].
Synonyms	MGCD265 hydrochloride

Chemical Properties

Molecular Weight	656.16
Formula	C₃₁H₂₈ClF₂N₅O₃S₂
Cas No.	1123838-51-6
Relative Density.	no data available

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: 28 mg/mL (42.67 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5240 mL	7.6201 mL	15.2402 mL	76.2009 mL
5 mM	0.3048 mL	1.5240 mL	3.0480 mL	15.2402 mL
10 mM	0.1524 mL	0.7620 mL	1.5240 mL	7.6201 mL
20 mM	0.0762 mL	0.3810 mL	0.7620 mL	3.8100 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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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