An inhibitor of Bcr-Abl
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PD 180970

Item No. 30619

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(2,6-dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
CAS Number
287204-45-9
Molecular Formula
C21H15Cl2FN4O
Formula Weight
429.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 20 mg/ml
SMILES
CC1=C(F)C=CC(NC2=NC=C(C=C(C3=C(Cl)C=CC=C3Cl)C(N4C)=O)C4=N2)=C1
InChi Code
InChI=1S/C21H15Cl2FN4O/c1-11-8-13(6-7-17(11)24)26-21-25-10-12-9-14(20(29)28(2)19(12)27-21)18-15(22)4-3-5-16(18)23/h3-10H,1-2H3,(H,25,26,27)
InChi Key
SLCFEJAMCRLYRG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $236

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    Product Description

    PD 180970 is an inhibitor of Bcr-Abl.1 It inhibits wild-type and mutant forms of Bcr-Abl, as well as the p210 isoform, a marker of chronic myelogenous leukemia (CML), with IC50 values ranging from 5 to 48 nM.1,2 PD 180970 is selective for Bcr-Abl over basic FGFR (bFGFR) and PDGFR (IC50s = 934 and 1,430 nM, respectively) but also inhibits Src, LCK, KIT, and EGFR (IC50s = 0.8, <5, 50, and 390 nM, respectively).3,4 It induces cell cycle arrest at the G1 phase and apoptosis in K562 CML cells when used at a concentration of 50 nM.5 PD 180970 (500 nM) inhibits constitutive STAT3 DNA-binding activity in, and proliferation of, MDA-MB-468 breast cancer cells.6 It also inhibits proliferation of Ba/F3 cells expressing mutant p210 Bcr-AblY253F that are resistant to imatinib (Item No. 13139) with an IC50 value of 48 nM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dorsey, J.F., Jove, R., Kraker, A.J., et al. The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 60(12), 3127-3131 (2000).

    2. La Rosée, P., Corbin, A.S., Stoffregen, E.P., et al. Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571). Cancer Res. 62(24), 7149-7153 (2002).

    3. 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).

    4. Corbin, A.S., Griswold, I.J., La Rosée, P., et al. Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood 104(12), 3754-3757 (2004).

    5. Huang, M., Dorsey, J.F., Epling-Burnette, P.K., et al. Inhibition of Bcr–Abl kinase activity by PD180970 blocks constitutive activation of Stat5 and growth of CML cells. Oncogene 21(57), 8804-8816 (2002).

    6. Garcia, R., Bowman, T.L., Niu, G., et al. Constitutive activation of Stat3 by the Src and JAK tyrosine kinases participates in growth regulation of human breast carcinoma cells. Oncogene 20(20), 2499-2513 (2001).