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XL228

Catalog No. T17267   CAS 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).

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XL228 Chemical Structure
XL228, CAS 898280-07-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
2 mg In stock $ 71.00
5 mg In stock $ 101.00
10 mg In stock $ 152.00
25 mg In stock $ 271.00
50 mg In stock $ 413.00
100 mg In stock $ 613.00
1 mL * 10 mM (in DMSO) In stock $ 112.00
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Purity: 98.92%
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Biological Description
Chemical Properties
Storage & Solubility Information
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].
Molecular Weight 437.54
Formula C22H31N9O
CAS No. 898280-07-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 83.33 mg/mL (190.45 mM)

TargetMolReferences and Literature

1. Cortes J, et al. Preliminary Clinical Activity in a Phase I Trial of the BCR-ABL/IGF- 1R/Aurora Kinase Inhibitor XL228 in Patients with Ph++ Leukemias with Either Failure to Multiple TKI Therapies or with T315I Mutation. Blood 2008 112:3232 2. Douglas O, et al. Abstract C192: Characterization of the target profile of XL228, a multi‐targeted protein kinase inhibitor in phase 1 clinical development. Mol Cancer Ther 2009;8(12 Suppl):C192. 3. Shah N, et al. Targeting Drug-Resistant CML and Ph+-ALL with the Spectrum Selective Protein Kinase Inhibitor XL228. Blood 2007 110:474;

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library ReFRAME Related Library Angiogenesis related Compound Library Cell Cycle Compound Library Epigenetics Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-Aging Compound Library

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Keywords

XL228 898280-07-4 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling Tyrosine Kinase/Adaptors IGF-1R Bcr-Abl Src Aurora Kinase Inhibitor XL 228 XL-228 inhibit inhibitor

 

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