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Zoligratinib

Chemical Structure : Zoligratinib

CAS No.: 1265229-25-1

Zoligratinib (Debio1347, CH5183284, Debio-1347, CH-5183284)

Catalog No.: PC-45761Not For Human Use, Lab Use Only.

CH-5183284 (Debio-1347, Debio1347) is a potent, selective and orally available FGFR1/2/3 inhibitor with enzyme IC50 of 9.3/7.6/22 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CH5183284 (Zoligratinib, Debio1347) is a potent, selective and orally available FGFR1/2/3 inhibitor with enzyme IC50 of 9.3/7.6/22 nM, respectively.
CH-5183284 displays >10-fold selectivity over FGFR4, and >100-fold over KDR, Src, and other kinases.
CH-5183284 displays preferential antitumor activity against cancer cells with various FGFR genetic alterations in a panel of 327 cancer cell lines and in xenograft models.
CH-5183284 can inhibit FGFR2 harboring one type of the gatekeeper mutation and blocks FGFR2 V564F-driven tumor growth.

Physicochemical Properties

M.Wt 356.3806
Formula C20H16N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 31mg/mL

Chemical Name/SMILES

Methanone, [5-amino-1-(2-methyl-1H-benzimidazol-6-yl)-1H-pyrazol-4-yl]-1H-indol-2-yl-

References

1. Ebiike H, et al. J Med Chem. 2016 Dec 8;59(23):10586-10600.

2. Nakanishi Y, et al. Mol Cancer Ther. 2014 Nov;13(11):2547-58.

3. Nakanishi Y, et al. Mol Cancer Ther. 2015 Dec;14(12):2831-9.

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