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| Cas No.: | 1265229-25-1 |
| Chemical Name: | Debio-1347 |
| Synonyms: | CH5183284;CH5183284 (Debio-1347);Debio 1347;DEBIO-1347;CH-5183284;FF284;NR9ZYH80Z8;(5-Amino-1-(2-methyl-1H-benzo[d]imidazol-6-yl)-1H-pyrazol-4-yl)(1H-indol-2-yl)methanone;[5-Amino-1-(2-Methyl-1h-Benzimidazol-6-Yl)-1h-Pyrazol-4-Yl](1h-Indol-2-Yl)methanone;BEMNJULZEQTDJY-UHFFFAOYSA-N;DEBIO1347;GTPL9787;BCP14354;BDBM50197683;s7665;DB12903;CS-5 |
| SMILES: | O=C(C1=C([H])C2=C([H])C([H])=C([H])C([H])=C2N1[H])C1C([H])=NN(C=1N([H])[H])C1C([H])=C([H])C2=C(C=1[H])N([H])C(C([H])([H])[H])=N2 |
| Formula: | C20H16N6O |
| M.Wt: | 356.3806 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | CH5183284 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. |
| In Vivo: | CH5183284 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. CH5183284 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]. |
| In Vitro: | CH5183284 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 CH5183284/Debio 1347 is 29 nM for FGF-dependent proliferation and 780 nM for VEGF-dependent proliferation[2]. |