CAS No. : 1265229-25-1

(Synonyms: Debio 1347; CH5183284)

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Cat. No. : HY-19957
M.Wt: 356.38
Formula: C20H16N6O
Purity: >98 %
Solubility: DMSO : 25 mg/mL (70.15 mM; ultrasonic and warming and heat to 50°C)
Introduction of 1265229-25-1 :

Zoligratinib (Debio 1347) is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. IC50 & Target: IC50: 9.3 nM (FGFR1), 7.6 nM (FGFR2), 22 nM (FGFR3), 290 nM (FGFR4)[1] In Vitro: Zoligratinib is well balanced in cellular antiproliferative activity against SNU-16 and stability in human liver microsome. The selectivity of 8 to inhibit FGFR over KDR is suggested to be caused by the difference in the interaction with M535 in FGFR1 and L889 in KDR[1]. The IC50 of Zoligratinib is 29 nM for FGF-dependent proliferation and 780 nM for VEGF-dependent proliferation[2]. In Vivo: Zoligratinib treatment shows a dose-dependent tumor regression (tumor growth inhibition (TGI)=106% at 30 mg/kg and 147% at 100 mg/kg) without apparent body weight loss. Zoligratinib treatment also shows significant in vivo efficacy in xenograft mice models with FGFR genetic alterations, such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), MFE280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion)[1].

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