Zoligratinib (Debio-1347)

For research use only.

Catalog No.S7665 Synonyms: CH5183284, FF284

6 publications

Zoligratinib (Debio-1347) Chemical Structure

CAS No. 1265229-25-1

Zoligratinib (Debio-1347, CH5183284, FF284) is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.

Selleck's Zoligratinib (Debio-1347) has been cited by 6 publications

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Biological Activity

Description Zoligratinib (Debio-1347, CH5183284, FF284) is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.
FGFR2 [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
FGFR4 [1]
(Cell-free assay)
7.6 nM 9.3 nM 22 nM 290 nM
In vitro

In cell-based assay, CH5183284 prevents autophosphorylation of FGFR1, FGFR2, and FGFR3 at 100 to 300 nM in the DMS114 (FGFR1 amplification), SNU-16 (FGFR2 amplification), and KMS11 [t(4;14) translocation and FGFR3 Y373C mutation] cell lines. CH5183284 thus produces selective antiproliferative activity against cancer cell lines harboring genetic alterations in FGFR. CH5183284 also inhibit FGFR2 harboring one type of the gatekeeper mutation (V564F) that causes resistance to other FGFR inhibitors. [1]

Methods Test Index PMID
Western blot
pERK / ERK / pAKT / AKT ; 

PubMed: 26438159     

Inhibition of ERK or AKT phosphorylation. After a 2-hour incubation with CH5183284/Debio 1347, cultures of DMS-114, NCI-H1581, SNU-16, KATO-III, SUM-52PE, UM-UC-14, and KMS-11 cells were lysed and analyzed by Western blotting. Ampli, amplification; mut, mutation.

DUSP6 ; 

PubMed: 26438159     

Inhibition of DUSP6 expression or ERK phosphorylation. After a 24-hour treatment with PD173074 (FGFR inhibitor) at 3 μmol/L or with PD0325901 (MEK inhibitor) at 1 μmol/L, cultures of NCI-H1581, DMS-114, AN3 CA, SNU-16, KMS-11, ZR-75-1, NCI-N87, and HCT116 cells were lysed and analyzed by Western blotting.

pY-FGFR / pY-KDR / pY-PDGFR / pY-c-KIT ; 

PubMed: 25169980     

Inhibition of cellular pY-FGFR1 in DMS-114 cells, pY-FGFR2 in SNU-16, pY-FGFR3 in KMS11, pY-FGFR4 in MDA-MB453, pY-KDR in HUVECs, pY-PDGFRα in NCI-H1703, and pY-cKIT in Kasumi-1 by CH5183284/Debio 1347 at the indicated concentration for 2 hours.

26438159 25169980
Growth inhibition assay
Cell viability ; 

PubMed: 25169980     

Cell growth inhibition of HUVECs by CH5183284/Debio 1347. HUVEC cells were seeded in medium containing VEGF (20 ng/mL) or ECGF (30 μg/mL) and treated with various concentrations of CH5183284/Debio 1347 for 4 days. Then, viable cells were counted with WST-8. Data are shown as mean ± SD (n = 3).

In vivo CH5183284 (100 mg/kg/day, p.o.) shows selective and significant antitumor activity against xenografts with FGFR genetic alterations such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), SNU-16 (gastric cancer, FGFR2 amplification), MFE-280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion). [1]


Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: 327 human tumor cell lines
  • Concentrations: ~10 μM
  • Incubation Time: 4 days
  • Method: 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)
Animal Research:[1]
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  • Animal Models: Mice bearing KG1, SNU-16, MFE280, UM-UC-14, RT112/84, or MKN-45 tumors
  • Dosages: 100 mg/kg/day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 71 mg/mL (199.22 mM)
Water Insoluble
Ethanol ''1 mg/mL warmed

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.38


CAS No. 1265229-25-1
Storage powder
in solvent
Synonyms CH5183284, FF284
Smiles CC1=NC2=C(N1)C=C(C=C2)N3C(=C(C=N3)C(=O)C4=CC5=CC=CC=C5N4)N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03834220 Active not recruiting Drug: Debio 1347 Solid Tumor Debiopharm International SA|Caris Life Sciences|Optimal Research (Just In Time sites) March 1 2019 Phase 2
NCT01948297 Terminated Drug: Debio1347 (CH5183284) Solid Tumours Debiopharm International SA August 2013 Phase 1

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FGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID