| Name | Zoligratinib |
| Description | Zoligratinib (CH5183284) is a selective and orally available FGFR inhibitor, which is for FGFR1(IC50=9.3 nM), FGFR2(IC50=7.6 nM), FGFR3(IC50=290), and FGFR4(IC50=22 nM), respectively. |
| Cell Research | The cell lines are added to the wells of 96-well plates containing 0.076 to 10,000 nM CH5183284/Debio 1347 and incubated at 37°C. After 4 days of incubation, Cell Counting Kit-8 solution is added and, after incubation for several more hours, absorbance at 450 nm is measured with the iMark Microplate-Reader. The antiproliferative activity is calculated using the formula (1 ? T/C) × 100 (%), where T and C represent absorbance at 450 nm of the cells treated with drugs (T) and that of untreated control cells (C). The IC50 values are calculated using Microsoft Excel 2007.(Only for Reference) |
| Kinase Assay | Protein kinase assay: The inhibitory activity of CH5183284/Debio 1347 against FGFR1 is evaluated using a radiometric filter assay by measuring the incorporation of 33Pi with a microplate scintillation counter. The phosphorylation activities of LCK, EGFR, KIT, MET, SRC, BRK, FGFR2, Flt3, LTK, INSR, YES, ABL, EPHA2, ZAP70, Fyn, IGF1R, KDR, and PDGFR on substrate peptides are determined by homogeneous time-resolved fluorescence assay with LANCE Eu-W1024 labeled anti-phosphotyrosine PT66 antibody according to standard methods. Time-resolved fluorescence is measured with an EnVision HTS microplate reader. The activities of Aurora A, Akt1/PKBα, PKA, Cdk1/cyclin B, Cdk2/cyclin A, PKCα, PKCβ1 and PKCβ2 on substrate peptides are determined by IMAP FP Screening Express Progressive Binding System. Fluorescence polarization is measured with an EnVision HTS microplate reader. |
| In vitro | In the DMS114 (FGFR1 amplification), SNU-16 (FGFR2 amplification), and KMS11 cell lines,CH5183284(100 to 300 nM) prevents autophosphorylation of FGFR1, FGFR2, and FGFR3. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 1 mg/mL (2.81 mM), Heating is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.61 mM), Sonication is recommended.
DMSO : 66 mg/mL (185.2 mM), Sonication is recommended.
|
| Keywords | Zoligratinib | Inhibitor | inhibit | Fibroblast growth factor receptor | FGFR4 | FGFR3 | FGFR2 | FGFR1 | FGFR | FF-284 | FF 284 | Debio-1347 | Debio1347 | CH-5183284 | CH 5183284 |
| Inhibitors Related | Amlexanox | Regorafenib monohydrate | Nintedanib | Ferulic Acid | Nintedanib esylate | Regorafenib | Pemigatinib | Formononetin | Lenvatinib mesylate | Erdafitinib | Lenvatinib | Pazopanib |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
