WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406350
Description: PD173074 is a small-molecule FGFR3-selective tyrosine kinase inhibitor (TKI), as a therapeutic modality using eight UC cell lines. PD173074 suppressed cell proliferation remarkably in two cell lines, namely, UM-UC-14 and MGHU3, which expressed mutated FGFR3 protein. Cell cycle analysis revealed the growth inhibitory effect of PD173074 was associated with arrest at G(1)-S transition in a dose-depending manner. In the mouse xenograft models using subcutaneously transplanted UM-UC-14 and MGHU3, orally administered PD173074 suppressed tumor growth and induced apoptotic changes comparable with the results of our in vitro assay.
MedKoo Cat#: 406350
Chemical Formula: C28H41N7O3
Exact Mass: 523.32709
Molecular Weight: 523.67024
Elemental Analysis: C, 64.22; H, 7.89; N, 18.72; O, 9.17
Synonym: PD173074; PD 173074; PD-173074.
IUPAC/Chemical Name: 1-(tert-butyl)-3-(2-((4-(diethylamino)butyl)amino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)urea
InChi Key: DXCUKNQANPLTEJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H41N7O3/c1-8-35(9-2)13-11-10-12-29-26-30-18-20-16-23(19-14-21(37-6)17-22(15-19)38-7)25(31-24(20)32-26)33-27(36)34-28(3,4)5/h14-18H,8-13H2,1-7H3,(H3,29,30,31,32,33,34,36)
SMILES Code: O=C(NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3)NC(C)(C)C
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs
Storage Condition: 0– 4 oC for short term (weeks to 1 month) or -20 C for long terms (months to years).
Solubility: soluble in DMSO, not soluble in water.
Shelf Life: >2 years if stored properly.
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 523.67024 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Ye YW, Hu S, Shi YQ, Zhang XF, Zhou Y, Zhao CL, Wang GJ, Wen JG, Zong H. Combination of the FGFR4 inhibitor PD173074 and 5-fluorouracil reduces proliferation and promotes apoptosis in gastric cancer. Oncol Rep. 2013 Dec;30(6):2777-84. doi: 10.3892/or.2013.2796. Epub 2013 Oct 11. PubMed PMID: 24126887.
2: Nguyen PT, Tsunematsu T, Yanagisawa S, Kudo Y, Miyauchi M, Kamata N, Takata T. The FGFR1 inhibitor PD173074 induces mesenchymal-epithelial transition through the transcription factor AP-1. Br J Cancer. 2013 Oct 15;109(8):2248-58. doi: 10.1038/bjc.2013.550. Epub 2013 Sep 17. PubMed PMID: 24045665; PubMed Central PMCID: PMC3798957.
3: Byron SA, Chen H, Wortmann A, Loch D, Gartside MG, Dehkhoda F, Blais SP, Neubert TA, Mohammadi M, Pollock PM. The N550K/H mutations in FGFR2 confer differential resistance to PD173074, dovitinib, and ponatinib ATP-competitive inhibitors. Neoplasia. 2013 Aug;15(8):975-88. PubMed PMID: 23908597; PubMed Central PMCID: PMC3730048.
4: Patel A, Tiwari AK, Chufan EE, Sodani K, Anreddy N, Singh S, Ambudkar SV, Stephani R, Chen ZS. PD173074, a selective FGFR inhibitor, reverses ABCB1-mediated drug resistance in cancer cells. Cancer Chemother Pharmacol. 2013 Jul;72(1):189-99. doi: 10.1007/s00280-013-2184-z. Epub 2013 May 15. PubMed PMID: 23673445.
5: Miyake M, Ishii M, Koyama N, Kawashima K, Kodama T, Anai S, Fujimoto K, Hirao Y, Sugano K. 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. 2010 Mar;332(3):795-802. doi: 10.1124/jpet.109.162768. Epub 2009 Dec 2. PubMed PMID: 19955487.
6: Pardo OE, Latigo J, Jeffery RE, Nye E, Poulsom R, Spencer-Dene B, Lemoine NR, Stamp GW, Aboagye EO, Seckl MJ. The fibroblast growth factor receptor inhibitor PD173074 blocks small cell lung cancer growth in vitro and in vivo. Cancer Res. 2009 Nov 15;69(22):8645-51. doi: 10.1158/0008-5472.CAN-09-1576. Epub 2009 Nov 10. PubMed PMID: 19903855.
7: Grand EK, Chase AJ, Heath C, Rahemtulla A, Cross NC. Targeting FGFR3 in multiple myeloma: inhibition of t(4;14)-positive cells by SU5402 and PD173074. Leukemia. 2004 May;18(5):962-6. PubMed PMID: 15029211.
8: Bansal R, Magge S, Winkler S. Specific inhibitor of FGF receptor signaling: FGF-2-mediated effects on proliferation, differentiation, and MAPK activation are inhibited by PD173074 in oligodendrocyte-lineage cells. J Neurosci Res. 2003 Nov 15;74(4):486-93. PubMed PMID: 14598292.
9: Dimitroff CJ, Klohs W, Sharma A, Pera P, Driscoll D, Veith J, Steinkampf R, Schroeder M, Klutchko S, Sumlin A, Henderson B, Dougherty TJ, Bernacki RJ. Anti-angiogenic activity of selected receptor tyrosine kinase inhibitors, PD166285 and PD173074: implications for combination treatment with photodynamic therapy. Invest New Drugs. 1999;17(2):121-35. PubMed PMID: 10638483.