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XL228

XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).

Catalog No. T17267Cas No. 898280-07-4

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Purity:99.07%

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XL228

Catalog No. T17267Cas No. 898280-07-4

XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).

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.

Pack Size	Price	Availability
1 mg	$51	In Stock
2 mg	$71	In Stock
5 mg	$101	In Stock
10 mg	$152	In Stock
25 mg	$271	In Stock
50 mg	$413	In Stock
100 mg	$613	In Stock
1 mL x 10 mM (in DMSO)	$112	In Stock

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Product Introduction

Bioactivity

Description	XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).
Targets&IC50	Aurora A:3.1 nM, IGF-1R:1.6 nM
In vitro	XL228 inhibits phosphorylation of BCR-ABL and its substrate STAT5 in K562 cells in vitro (IC50s: 33 and 43 nM, respectively). XL228 eliminates the phosphorylation of Aurora A and B at concentrations above 10 nM. XL228 displays a broad pattern of protein kinase inhibition, including the tyrosine kinases IGF1R, SRC, ABL, FGFR1-3, and ALK and the serine/threonine kinases Aurora A and Aurora B. Approximately 30% of the lines demonstrate XL228 IC50 values of <100nM in viability assays, including many lines with characterized ALK or FGFR mutations or amplifications [2][3].
In vivo	Single-dose pharmacodynamics studies demonstrate that XL228 on BCR-ABL signaling in K562 xenograft tumors has a potent effect. At XL228 plasma concentrations of 3.5 μM, phosphorylation of BCR-ABL is decreased by 50%; a similar decrease in phospho-STAT5 occurred at 0.8 μM plasma concentration [3].

Chemical Properties

Molecular Weight	437.54
Formula	C₂₂H₃₁N₉O
Cas No.	898280-07-4

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 83.33 mg/mL (190.45 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2855 mL	11.4275 mL	22.8551 mL	114.2753 mL
5 mM	0.4571 mL	2.2855 mL	4.5710 mL	22.8551 mL
10 mM	0.2286 mL	1.1428 mL	2.2855 mL	11.4275 mL
20 mM	0.1143 mL	0.5714 mL	1.1428 mL	5.7138 mL
50 mM	0.0457 mL	0.2286 mL	0.4571 mL	2.2855 mL
100 mM	0.0229 mL	0.1143 mL	0.2286 mL	1.1428 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:

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

DMSO+30% PEG300+5% Tween 80+60% 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

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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 μLddH2O TargetMol | reagent

mix well and clarify

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

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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