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製品名PD 173074, FGFR1 and FGFR3 inhibitor
製品の詳細Potent FGFR1 and FGFR3 inhibitor
生理活性の詳細Potent, ATP-competitive fibroblast growth factor receptor 1 (FGFR1) and FGFR3 inhibitor (IC50 values are 21.5 and 5 nM respectively). Shows little activity at EGFR, InsR, MEK and cPKC. Effectively inhibits angiogenesis in vivo. Also impairs tumor growth and inhibits self-renewal of stem cells.
保存方法Store at +4°C. The product can be stored for up to 12 months.
溶解性Soluble in DMSO to 100 mM and in ethanol to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Our Abpromise guarantee covers the use of ab141117 in the following tested applications.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
|Functional Studies||Use at an assay dependent concentration.|
BT549 cells were incubated at 37ºC for 1 hour with vehicle control (0 µM) and different concentrations of PD 173074 (ab141117) in DMSO. Decreased expression of RSK1 p90 (phospho T359 + S363) ab32413 correlates with an increase in PD 173074 concentration, as described in literature.
Whole cell lysates were prepared with RIPA buffer (containing protease inhibitors and sodium orthovanadate), 10 µg of each were loaded on the gel and the WB was run under reducing conditions. After transfer the membrane was blocked for an hour using 5% BSA before being incubated with ab32413 at 1/5000 dilution and ab8227 at 1 μg/ml overnight at 4°C. Antibody binding was detected using an anti-rabbit antibody conjugated to HRP ab97051 at 1/10000 dilution and visualised using ECL development solution.
This product has been referenced in:
- Miyake M et al. 1-tert-butyl-3-[6-(3,5-dimethoxy-phenyl)-2-(4-diethylamino-butylamino)-pyrido[2,3-d]pyrimidin-7-yl]-urea (PD173074), a selective tyrosine kinase inhibitor of fibroblast growth factor receptor-3 (FGFR3), inhibits cell proliferation of bladder cancer carrying the FGFR3 gene mutation along with up-regulation of p27/Kip1 and G1/G0 arrest. J Pharmacol Exp Ther 332:795-802 (2010). Read more (PubMed: 19955487) »
- Pardo OE et al. The fibroblast growth factor receptor inhibitor PD173074 blocks small cell lung cancer growth in vitro and in vivo. Cancer Res 69:8645-51 (2009). Read more (PubMed: 19903855) »
- Zaragosi LE et al. Autocrine fibroblast growth factor 2 signaling is critical for self-renewal of human multipotent adipose-derived stem cells. Stem Cells 24:2412-9 (2006). Read more (PubMed: 16840552) »
- Mohammadi M et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J 17:5896-904 (1998). Read more (PubMed: 9774334) »