XL228

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

Product Specifications

CAS Number

[898280-07-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Aurora Kinase; Bcr-Abl; IGF-1R; Src

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Endocrinology

Assay Protocol

https://www.medchemexpress.com/XL228.html

Purity

99.64

Solubility

DMSO : ≥ 83.33 mg/mL

Smiles

CN1CCN(C2=CC(NC3=NNC(C4CC4)=C3)=NC(NCC5=CC(C(C)C)=NO5)=N2)CC1

Molecular Formula

C22H31N9O

Molecular Weight

437.54

Precautions

H302, H315, H319

References & Citations

[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