PD 173955

PD 173955 is a tyrosine kinase inhibitor.^1,2 It inhibits c-Src, Yes, and LCK (IC₅₀s = 25, 22, and 5 nM, respectively), as well as Bcr-Abl and c-Kit (IC₅₀s = 1-2 and 25 nM, respectively), and is selective for these kinases over the insulin receptor (InsR), α-FGFR, basic FGFR (bFGFR), PDGFR, and PKC.^3,1,2 PD 173955 (5,000 nM) induces cell cycle arrest at the G₂/M phase in DU145 prostate, SKOV3 ovarian, HT-29 colon, A549 lung, and A431 skin cancer cells.¹ It inhibits proliferation of MDA-MB-468 and MCF-7 breast cancer cells (IC₅₀s = 500 and 1,000 nM, respectively), as well as patient-derived peripheral blood chronic myelogenous leukemia (CML) progenitor cells (IC₅₀= ~7.5 nM).^1,2

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1. Moasser, M.M., Srethapakdi, M., Sachar, K.S., et al. Inhibition of Src kinases by a selective tyrosine kinase inhibitor causes mitotic arrest. Cancer Res. 59(24), 145-152 (1999).

2. Wisniewski, D., Lambek, C.L., Liu, C., et al. Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinases. Cancer Res. 62(15), 4244-4255 (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).