Infigratinib phosphate, Inhibitor

Infigratinib phosphate

Cat. Num. AAA5755292

• Purity: 98.00%
• Synonyms: Infigratinib phosphate; BGJ-398 phosphate; NVP-BGJ398 phosphate; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• Formula: C26H34Cl2N7O7P
• SMILES: O=P(O)(O)O.ClC1=C(C(Cl)=C(C=C1OC)OC)NC(N(C2=CC(NC3=CC=C(C=C3)N4CCN(CC4)CC)=NC=N2)C)=O
• CAS Number: 1310746-10-1
• Target & IC50: FGFR1: ic50 0.9nM; FGFR2: ic50 1.4nM; FGFR3: ic50 1nM; FGFR4: ic50 60nM
• In Vitro: Infigratinib (30mg/kg) significantly suppresses the growth of FGFR2-mutated endometrial cancer xenograft models. Infigratinib is administered to athymic nude mice implanted subcutaneously with RT112/luc1 tumors: either as a 5mg/kg intravenous bolus innMP/PEG200 (1:9, v/v) or orally by gavage as a suspension in PEG300/D5W (2:1, v/v) at a 20mg/kg dose. Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues after intravenous dosing, translating into a high volume of distribution (26L/kg). The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. The plasma clearance is high at 3.3L/h/kg (61% of liver blood flow). The ratio of tumor to plasma after oral dosing based on AUC is determined to be 10 [1][2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Infigratinib phosphate, inhibitor

Infigratinib phosphate is an effective inhibitor of the FGFR family (IC50: 0.9nM, 1.4nM, 1nM, and 60nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively).

Product Categories/Family for Infigratinib phosphate, inhibitor

Angiogenesis; Tyrosine Kinase/Adaptors

References

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-me thyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor T
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-me thyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor T
Konecny GE, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42.
Konecny GE, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42.