A tyrosine kinase inhibitor
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XL228

Item No. 21506

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-[[3-(1-methylethyl)-5-isoxazolyl]methyl]-6-(4-methyl-1-piperazinyl)-2,4-pyrimidinediamine
CAS Number
898280-07-4
Molecular Formula
C22H31N9O
Formula Weight
437.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 16.67 mg/ml
λmax
236, 291 nm
SMILES
CN1CCN(C2=CC(NC3=NNC(C4CC4)=C3)=NC(NCC5=CC(C(C)C)=NO5)=N2)CC1
InChi Code
InChI=1S/C22H31N9O/c1-14(2)17-10-16(32-29-17)13-23-22-25-19(24-20-11-18(27-28-20)15-4-5-15)12-21(26-22)31-8-6-30(3)7-9-31/h10-12,14-15H,4-9,13H2,1-3H3,(H3,23,24,25,26,27,28)
InChi Key
ALKJNCZNEOTEMP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $158

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    25 mg

    $354

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    50 mg

    $634

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    Product Description

    XL228 is a tyrosine kinase inhibitor.1,2 It inhibits the receptor tyrosine kinases insulin-like growth factor 1 receptor (IGF-1R) and FGFR2 (IC50s = 1.6 and <20 nM, respectively), as well as the non-receptor tyrosine kinases Bcr-Abl, Aurora A, LYN, and Src (IC50s = 5, 3.1, 2, and 6.1 nM, respectively). XL228 inhibits proliferation of chronic myelogenous leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines (IC50s = <100 nM).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cortes, J., Paquette, R., Talpaz, M., 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 112(11), 3232 (2008).

    2. Clary, D.O., Ollmann, M.M., Detmer, S.A., 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. 8(12 Suppl), C192 (2009).

    3. Shah, N.P., Kasap, C., Paquette, R., et al. Targeting drug-resistant CML and Ph+-ALL with the spectrum selective protein kinase inhibitor XL228. Blood 110(11), 474 (2007).