Description
CH5183284 (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.
Product information
CAS Number: 1265229-25-1
Molecular Weight: 356.38
Formula: C20H16N6O
Chemical Name: 4-(1H-indole-2-carbonyl)-1-(2-methyl-1H-1,3-benzodiazol-6-yl)-1H-pyrazol-5-amine
Smiles: CC1NC2=CC(=CC=C2N=1)N1N=CC(=C1N)C(=O)C1=CC2C=CC=CC=2N1
InChiKey: BEMNJULZEQTDJY-UHFFFAOYSA-N
InChi: InChI=1S/C20H16N6O/c1-11-23-16-7-6-13(9-17(16)24-11)26-20(21)14(10-22-26)19(27)18-8-12-4-2-3-5-15(12)25-18/h2-10,25H,21H2,1H3,(H,23,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 25 mg/mL (70.15 mM; ultrasonic and warming and heat to 50°C).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. The IC50 of CH5183284/Debio 1347 is 29 nM for FGF-dependent proliferation and 780 nM for VEGF-dependent proliferation.
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).
Products are for research use only. Not for human use.
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