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PD 173074

Cayman Chemical Item Number 13032

(CAS 219580-11-7)

PD 173074 (CAS 219580-11-7)

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Description

The fibroblast growth factor receptors (FGFRs) are cell surface receptors with intrinsic tyrosine kinase activity, which is necessary for receptor activation and signal propagation. PD 173074 is a potent and selective inhibitor of FGFR tyrosine kinase activity, blocking autophosphorylation of FGFR1 with an IC50 value of 21.5 nM.1 For comparison, it weakly inhibits PDGFR and c-Src (IC50 = 17.6 and 19.8 μM, respectively) and has no effect on EGFR, InsR, MEK, or PKC.1 PD 173074 also prevents signaling, at nanomolar levels, through FGFR2-5.2,3,4,5,6 Inhibition of FGFR signaling using PD 173074, impairs angiogenesis5,2 as well as self-renewal of stem cells via ERK1/2 activation.7,8,6

1 Mohammadi, M., Froum, S., Hamby, J.M., et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J 17(20) 5896-5904 (1998).

2 Skaper, S.D., Kee, W.J., Facci, L., et al. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J Neurochem 75 1520-1527 (2000).

3 Koziczak, M., Holbro, T., and Hynes, N.E. Blocking of FGFR signaling inhibits breast cancer cell proliferation through downregulation of D-type cyclins. Oncogene 23 3501-3508 (2004).

4 Grand, E.K., Chase, A.J., Heath, C., et al. Targeting FGFR3 in multiple myeloma: inhibition of t(4;14)-positive cells by SU5402 and PD173074. Leukemia 18 962-966 (2004).

5 St.Bernard, R., Zheng, L., Liu, W., et al. Fibroblast growth factor receptors as molecular targets in thyroid carcinoma. Endocrinology 146(3) 1145-1153 (2005).

6 Stavridis, M.P., Lunn, J.S., Collins, B.J., et al. A discrete period of FGF-induced Erk1/2 signalling is required for vertebrate neural specification. Development 134 2889-2894 (2007).

7 Kunath, T., Saba-El-Leil, M.K., Almousailleakh, M., et al. FGF stimulation of the Erk1/2 signalling cascade triggers transition of pluripotent embryonic stem cells from self-renewal to lineage commitment. Development 134 2895-2902 (2007).

8 Zaragosi, L., Ailhaud, G., and Dani, C. Autocrine fibroblast growth factor 2 signaling is critical for self-renewal of human multipotent adipose-derived stem cells. Stem Cells 24 2412-2419 (2006).

Formal Name N-​[2-​[[4-​(diethylamino)butyl]amino]-​6-​(3,​5-​dimethoxyphenyl)pyrido[2,​3-​d]pyrimidin-​7-​yl]-​N'-​(1,​1-​dimethylethyl)-​urea
CAS Number 219580-11-7
Molecular Formula C28H41N7O3
Formula Weight 523.7
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CCN(CC)​CCCCNc1ncc2cc(c3cc(OC)​cc(OC)​c3)​c(NC(=O)​NC(C)​(C)​C)​nc2n1

Background Reading

Zaragosi, L., Ailhaud, G., and Dani, C. Autocrine fibroblast growth factor 2 signaling is critical for self-renewal of human multipotent adipose-derived stem cells. Stem Cells 24 2412-2419 (2006).

Kunath, T., Saba-El-Leil, M.K., Almousailleakh, M., et al. FGF stimulation of the Erk1/2 signalling cascade triggers transition of pluripotent embryonic stem cells from self-renewal to lineage commitment. Development 134 2895-2902 (2007).

Stavridis, M.P., Lunn, J.S., Collins, B.J., et al. A discrete period of FGF-induced Erk1/2 signalling is required for vertebrate neural specification. Development 134 2889-2894 (2007).

St.Bernard, R., Zheng, L., Liu, W., et al. Fibroblast growth factor receptors as molecular targets in thyroid carcinoma. Endocrinology 146(3) 1145-1153 (2005).

Grand, E.K., Chase, A.J., Heath, C., et al. Targeting FGFR3 in multiple myeloma: inhibition of t(4;14)-positive cells by SU5402 and PD173074. Leukemia 18 962-966 (2004).

Koziczak, M., Holbro, T., and Hynes, N.E. Blocking of FGFR signaling inhibits breast cancer cell proliferation through downregulation of D-type cyclins. Oncogene 23 3501-3508 (2004).

Mohammadi, M., Froum, S., Hamby, J.M., et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J 17(20) 5896-5904 (1998).

Skaper, S.D., Kee, W.J., Facci, L., et al. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J Neurochem 75 1520-1527 (2000).

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PD 173074 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $21.00 $0.00
5 mg $88.00 $0.00
10 mg $154.00 $0.00
25 mg $263.00 $0.00
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Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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