Zoligratinib

SKU: orb1301141

Description

Zoligratinib (CH5183284) is an orally bioavailable, selective FGFR inhibitor with IC50 values of 9.3 nM (FGFR1), 7.6 nM (FGFR2), 22 nM (FGFR4), and 290 nM (FGFR3). It is a research tool used in vitro and in vivo to study FGFR-driven oncogenesis and targeted therapy in cancers such as urothelial carcinoma.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1265229-25-1
• MW: 356.38
• Purity: 99.51% (May vary between batches)
• Formula: C₂₀H₁₆N₆O
• SMILES: Cc1nc2ccc(cc2[nH]1)-n1ncc(C(=O)c2cc3ccccc3[nH]2)c1N
• Target: FGFR
• Solubility: Ethanol:1 mg/mL (2.81 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.61 mM);DMSO:66 mg/mL (185.2 mM)

Bioactivity

• Target IC50:
  FGFR1:9.3 nM|FGFR3:22 nM|FGFR4:290 nM|FGFR2:7.6 nM
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CH5183284, CH-5183284, CH 5183284, Inhibitor, FGFR1, FGFR, FF 284, FF284, FF-284, Fibroblast growth factor receptor, FGFR2, FGFR3, FGFR4, Debio1347, Debio-1347, Debio 1347, inhibit, Zoligratinib

Compound Identifiers

PubChem CID

66555680