BGJ-398 is a pan FGFR kinase inhibitor, and is an orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. pan FGFR kinase inhibitor BGJ398 selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death.
Chemical Formula: C26H31Cl2N7O3
Exact Mass: 559.18654
Molecular Weight: 560.47
Elemental Analysis: C, 55.72; H, 5.57; Cl, 12.65; N, 17.49; O, 8.56
Appearance: White to off-white 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: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not 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
Infigratinib (BGJ-398) inhibits FGFR1, FGFR2, and FGFR3 with IC50=~1 nM, FGFR3K650E with IC50=4.9 nM, and FGFR4 with IC50=60 nM. IC50 values for all other kinases are in the μM range (FYN, LCK, YES, and ABL, IC50=1.9, 2.5, 1.1, and 2.3 μM, respectively) except for VEGFR2, KIT, and LYN, which are inhibited at submicromolar concentrations (IC50=0.18, 0.75, and 0.3 μM, respectively).
Infigratinib (BGJ-398) inhibits the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values which are in the low nanomolar range and comparable to those observed for the inhibition of the receptors kinase activity in the enzymatic assay.
For the remaining cells, all IC50 values are greater than 1.5 μM except for VEGFR2 (IC50 1449 and 938 nM), for which there is at least a 400-fold selectivity versus FGFR1, FGFR2, and FGFR3.
Infigratinib (BGJ-398) (ranging between 1 nM and 10 μM) is potent at inhibiting cell growth of FGFR2-mutant endometrial cancer cells.
Infigratinib (BGJ-398) is administered to athymic nude mice implanted subcutaneously with RT112/luc1 tumors: either as a 5 mg/kg intravenous bolus in NMP/PEG200 (1:9, v/v) or orally by gavage as a suspension in PEG300/D5W (2:1, v/v) at a 20 mg/kg dose.The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib (BGJ-398) in this study is 32%. After intravenous dosing, Infigratinib (BGJ-398) shows a rapid distribution from the vascular compartment into the peripheral tissues, translating into a high volume of distribution (26 L/kg). The plasma clearance is high at 3.3 L/h/kg (61% of liver blood flow). The ratio of tumor to plasma after oral dosing based on AUC is determined to be 10.
Infigratinib (BGJ-398) (30 mg/kg) significantly inhibits the growth of FGFR2-mutated endometrial cancer xenograft models.
Tran A, Koh TS, Prawira A, Ho RZW, Le TBU, Vu TC, Hartano S, Teo XQ, Chen WC, Lee P, Thng CH, Huynh H. Dynamic Contrast-Enhanced Magnetic Resonance Imaging as Imaging Biomarker for Vascular Normalization Effect of Infigratinib in High- FGFR-Expressing Hepatocellular Carcinoma Xenografts. Mol Imaging Biol. 2020 Sep 9. doi: 10.1007/s11307-020-01531-7. Epub ahead of print. PMID: 32909245.
Magone MT, Hartley IR, Fitzgibbon E, Bishop R, Arango M, Moran S, Vold R, Rivero JD, Pozo K, Streit J, Roszko KL, Collins MT, Gafni RI. Ocular Adverse Effects of Infigratinib, a New Fibroblast Growth Factor Receptor Tyrosine Kinase Inhibitor. Ophthalmology. 2020 Sep 1:S0161-6420(20)30844-7. doi: 10.1016/j.ophtha.2020.08.026. Epub ahead of print. PMID: 32888946.
Lyou Y, Grivas P, Rosenberg JE, Hoffman-Censits J, Quinn DI, P Petrylak D, Galsky M, Vaishampayan U, De Giorgi U, Gupta S, Burris H, Rearden J, Li A, Wang H, Reyes M, Moran S, Daneshmand S, Bajorin D, Pal SK. Hyperphosphatemia Secondary to the Selective Fibroblast Growth Factor Receptor 1-3 Inhibitor Infigratinib (BGJ398) Is Associated with Antitumor Efficacy in Fibroblast Growth Factor Receptor 3-altered Advanced/Metastatic Urothelial Carcinoma. Eur Urol. 2020 Aug 23:S0302-2838(20)30616-3. doi: 10.1016/j.eururo.2020.08.002. Epub ahead of print. PMID: 32847703.
Makawita S, K Abou-Alfa G, Roychowdhury S, Sadeghi S, Borbath I, Goyal L, Cohn A, Lamarca A, Oh DY, Macarulla T, T Shroff R, Howland M, Li A, Cho T, Pande A, Javle M. Infigratinib in patients with advanced cholangiocarcinoma with FGFR2 gene fusions/translocations: the PROOF 301 trial. Future Oncol. 2020 Jun 25. doi: 10.2217/fon-2020-0299. Epub ahead of print. PMID: 32580579.
Pal SK, Bajorin D, Dizman N, Hoffman-Censits J, Quinn DI, Petrylak DP, Galsky MD, Vaishampayan U, De Giorgi U, Gupta S, Burris HA, Soifer HS, Li G, Wang H, Dambkowski CL, Moran S, Daneshmand S, Rosenberg JE. Infigratinib in upper tract urothelial carcinoma versus urothelial carcinoma of the bladder and its association with comprehensive genomic profiling and/or cell-free DNA results. Cancer. 2020 Jun 1;126(11):2597-2606. doi: 10.1002/cncr.32806. Epub 2020 Mar 24. PMID: 32208524; PMCID: PMC7515773.
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