[CAS NO. 1265229-25-1] Zoligratinib (Debio-1347)
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PRODUCTS SPECIFICATIONS [1265229-25-1]
Catalog
SLK-S7665
Brand
Selleck
CAS
1265229-25-1
DESCRIPTION [1265229-25-1]
Overview
| MDL | MFCD28502053 |
|---|---|
| Molecular Weight | 356.38 |
| Molecular Formula | C20H16N6O |
| SMILES | O=C(C1=C(N)N(C2=CC=C3C(NC(C)=N3)=C2)N=C1)C(N4)=CC5=C4C=CC=C5 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8060 mL | 14.0300 mL | 28.0599 mL |
| 5 mM | 0.5612 mL | 2.8060 mL | 5.6120 mL |
| 10 mM | 0.2806 mL | 1.4030 mL | 2.8060 mL |
| 50 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL |
Description
Zoligratinib (Debio-1347, CH5183284, FF284) is a selective and orally available inhibitor with of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.
Targets
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.
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).
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