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PD 173074

Cayman Chemical Item Number 13032

(CAS 219580-11-7)

PD 173074 (CAS 219580-11-7)

See more	Inhibitors (493) Cancer (606) Cell Biology (281) Signal Transduction (314) Stem Cell Research (23)

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 angiogenesis^5,2 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	Copy SMILES to clipboard 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:

Bio-active Lipid I Screening Library (96-Well)

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
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-12. 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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