Infigratinib free basefeatured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:204640
CAS#:872511-34-7 (free base)
Description:Infigratinib, also known as, BGJ398 or NVP-BGJ398, 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.
Price and Availability
Infigratinib free base, purity > 98%, is in stock. The same day shipping out after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 204640Name: Infigratinib free baseCAS#: 872511-34-7 (free base)Chemical Formula: C26H31Cl2N7O3Exact Mass: 559.18654Molecular Weight: 560.47Elemental Analysis:C, 55.72; H, 5.57; Cl, 12.65; N, 17.49; O, 8.56
Related CAS #:872511-34-7 (free base)1310746-10-1 (phosphate)1310746-11-2 (monohydrate)1310746-12-3 (mesylate)
Synonym:NVPBGJ398; NVPBGJ 398; NVPBGJ-398; BGJ398; BGJ-398; BG J398; Infigratinib.
IUPAC/Chemical Name:3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea.
InChi Key:QADPYRIHXKWUSV-UHFFFAOYSA-N
InChi Code:InChI=1S/C26H31Cl2N7O3/c1-5-34-10-12-35(13-11-34)18-8-6-17(7-9-18)31-21-15-22(30-16-29-21)33(2)26(36)32-25-23(27)19(37-3)14-20(38-4)24(25)28/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31)
SMILES Code:O=C(NC1=C(Cl)C(OC)=CC(OC)=C1Cl)N(C2=NC=NC(NC3=CC=C(N4CCN(CC)CC4)C=C3)=C2)C
Technical Data
Additional Information
BGJ398 is a potent, selective and orally active pan-FGFR inhibitor, with IC50s of 0.9, 1.4, 1.0 and 60 nM for FGFR1, 2, 3 and 4, respectively.
CAS#872511-34-7 ( BGJ-398 free base); 1310746-11-2 (BGJ-398 monohydrate); 1310746-10-1 (BGJ-398 phosphate salt)
References
1: 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.
2: 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.
3: 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.
4: 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.
5: 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.
6: Felix NS, de Mendonça L, Braga CL, da Silva JS, Samary CDS, Vieira JB, Cruz F, Rocha NN, Zapata-Sudo G, Rocco PRM, Silva PL. Effects of the FGF receptor-1 inhibitor, infigratinib, with or without sildenafil, in experimental pulmonary arterial hypertension. Br J Pharmacol. 2019 Dec;176(23):4462-4473. doi: 10.1111/bph.14807. Epub 2019 Dec 5. PMID: 31351013; PMCID: PMC6932937.
7: Huynh H, Lee LY, Goh KY, Ong R, Hao HX, Huang A, Wang Y, Graus Porta D, Chow P, Chung A. Infigratinib Mediates Vascular Normalization, Impairs Metastasis, and Improves Chemotherapy in Hepatocellular Carcinoma. Hepatology. 2019 Mar;69(3):943-958. doi: 10.1002/hep.30481. PMID: 30575985; PMCID: PMC6635738.
