A multi-kinase inhibitor
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PD 173952

Item No. 45469

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(2,6-dichlorophenyl)-8-methyl-2-[[4-(4-morpholinyl)phenyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one
CAS Number
305820-75-1
Molecular Formula
C24H21Cl2N5O2
Formula Weight
482.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C1C(C2=C(C=CC=C2Cl)Cl)=CC3=C(N1C)N=C(NC4=CC=C(N5CCOCC5)C=C4)N=C3
InChi Code
InChI=1S/C24H21Cl2N5O2/c1-30-22-15(13-18(23(30)32)21-19(25)3-2-4-20(21)26)14-27-24(29-22)28-16-5-7-17(8-6-16)31-9-11-33-12-10-31/h2-8,13-14H,9-12H2,1H3,(H,27,28,29)
InChi Key
XZEJMVDCQZRHLN-UHFFFAOYSA-N
Origin
Synthetic
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $27

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    PD 173952 is a multi-kinase inhibitor.1,2 It inhibits LYN, Abl, CSK, and c-Src in cell-free assays (IC50s = 0.3, 1.7, 6.6, and 8.5 nM, respectively. PD 173952 inhibits the growth of HCT-8, SW620, and HT-29 colon carcinoma cells (IC50s = 1.53, 1.8, and 0.526 µM, respectively).1 It induces cell cycle arrest at the G2/M phase in HT-29 cells when used at a concentration of 1 µM. PD 173952 (0.5 µM) induces apoptosis in K562 and MEG-01 chronic myeloid leukemia cells.2 It also inhibits ristocetin-induced aggregation in human platelet-rich plasma.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kraker, A.J., Hartl, B.G., Amar, A.M., et al. Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem. Pharmacol. 60(7), 885-898 (2000).

    2. Dorsey, J.F., Cunnick, J.M., Lanehart, R., et al. Interleukin-3 protects Bcr-Abl-transformed hematopoietic progenitor cells from apoptosis induced by Bcr-Abl tyrosine kinase inhibitors. Leukemia 16(9), 1589-1595 (2002).

    3. Marshall, S.J., Senis, Y.A., Auger, J.M., et al. GPIb-dependent platelet activation is dependent on Src kinases but not MAP kinase or cGMP-dependent kinase. Blood 103(7), 2601-2609 (2004).