I-1500 Infigratinib, Free Base, >99%

Synonyms : [BGJ398] [NVPBGJ398]

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  • 5 mg
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  • 10 mg
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  • 25 mg
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  • 50 mg
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  • 100 mg
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  • 200 mg
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  • 396
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  • 500 mg
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  • 1 g
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  • 1,024
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  • M.W. 560.48
  • C26H31Cl2N7O3
  • [872511-34-7]

Solubility: Soluble in DMSO.

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  • Infigratinib, also known as BGJ398, is a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinases. It was shown to have significant antitumor activity in RT112 bladder cancer xenografts models that overexpress wild-type FGFR3. Guagnano, V. et al., "Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase." J. Med. Chem. 54: 7066-7083 (2011).
  • This research compound is the free base form of infigratinib. We also plan to offer the phosphate salt form, Cat. No. I-1533, Infigratinib, Phosphate Salt. The phosphate salt form will be added to our website as soon as the first lot is ready for shipment.
  • Infigratinib inhibited FGFR1, FGFR2, and FGFR3 with single digit nM IC50 potencies in biochemical and cellular autophosphorylation assays. It significantly blocked proliferation of cancer cell lines bearing FGF/FGFR genetic alterations across various cancer types. Guagnano, V. et al., "FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor." Cancer Discov. 2: 1118-1133 (2012).
  • Infigratinib inhibited FGFR2 signaling, induced cell-cycle arrest, and significantly increased apoptosis in FGFR2-mutant lines. It inhibited the proliferation of cancer cell lines with activating FGFR2 mutations (S252W, N550K) more effectively compared to their FGFR2 wild-type counterparts in vitro. It also blocked the growth of FGFR2-mutated endometrial cancer xenograft models more effectively compared to the wild type tumors in vivo. Konecny, G.E. et al., "Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells." Mol. Cancer Ther. 12: 632-642 (2013).
  • This infigratinib product is the free base form, whose CAS number is given above. The CAS number for the phosphate salt is 1310746-10-1.
  • Related CAS numbers: 1310746-12-3 for the (1:1) methanesulfonate salt; 1310746-11-2 for the (1:1) hydrate; 1310746-17-8 for the (1:1) acetate salt; 1310746-15-6 for the (1:1) hydrochloride salt; 1310746-16-7 for the (1:1:2) hydrochloride dihydrate salt; 1310746-20-3 for the (1:1) fumarate salt; 1310746-19-0 for the (1:1) citrate salt; and 1310746-18-9 for the (1:1) benzoate salt.
  • Another CAS number previously assigned to Infigratinib, Free Base, namely 1430224-87-5, has been deleted by CAS and is no longer in use.
  • 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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