A-1088 AZD4547, Free Base, >99%

  • Size
  • US $
  • £
  • ¥
  • 5 mg
  • 42
  • 35
  • 32
  • 4,700
  • Add to Cart Qty:
  • In stock
  • 10 mg
  • 51
  • 43
  • 38
  • 5,700
  • Add to Cart Qty:
  • In stock
  • 25 mg
  • 84
  • 71
  • 64
  • 9,300
  • Add to Cart Qty:
  • In stock
  • 50 mg
  • 114
  • 97
  • 87
  • 12,700
  • Add to Cart Qty:
  • In stock
  • 100 mg
  • 178
  • 152
  • 135
  • 19,800
  • Add to Cart Qty:
  • In stock
  • 200 mg
  • 272
  • 232
  • 207
  • 30,200
  • Add to Cart Qty:
  • In stock

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  • M.W. 463.57
  • C26H33N5O3
  • [1035270-39-3]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 90 mg/mL; soluble in ethanol at 25 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 25-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

Certificate of Analysis

  • AZD4547 is a novel and selective inhibitor of the fibroblast growth factor receptor (FGFR) 1, 2, and 3 tyrosine kinases. It potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, and 3 in vitro with IC50 values of 0.2, 2.5, and 1.8 nM, respectively. In cells, it inhibited autophosphorylation of FGFR1, 2, and 3 tyrosine kinases with IC50 values of 12, 2, and 40 nM, respectively. It had potent antitumor activity against FGFR-deregulated tumors in preclinical models. Gavine, P.R., et al. "AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family." Cancer Res. 72: 2045-2056 (2012).
  • AZD4547 inhibited the growth of gastric cancer cell lines SNU-16 and KATO-III, carrying the amplified FGFR2 gene, with GI50 values of 3 and 5 nM, respectively. It also effectively inhibited phosphorylation of FGFR2 and its downstream signaling molecules and resulted in apoptosis in SNU-16 cells. Furthermore, it significantly inhibited the tumor growth in FGFR2-amplified xenograft (SNU-16) and PDGCX models (SGC083) but not in nonamplified models. Xie, L., et al. "FGFR2 gene amplification in gastric cancer predicts sensitivity to the selective FGFR inhibitor AZD4547." Clin. Cancer Res. 19: 2572-2583 (2013).
  • AZD4547 inhibited the cell growth only in those lines harboring amplified FGFR1 with GI50 values of 3-111 nM. AZD4547 caused tumor stasis or regressive effects in four of five FGFR1-amplified squamous non-small cell lung cancer patient-derived tumor xenograft models. Zhang, J., et al. "Translating the therapeutic potential of AZD4547 in FGFR1-amplified non-small cell lung cancer through the use of patient-derived tumor xenograft models." Clin. Cancer Res. 18: 6658-6667 (2012).
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.
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