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ONO-4059 hydrochloride

Chemical Structure : ONO-4059 hydrochloride

CAS No.: 1439901-97-9

ONO-4059 hydrochloride (ONO4059 hydrochloride;Tirabrutinib hydrochloride;GS4059 hydrochloride;GS 4059 hydrochloride;GS-4059 hydrochloride)

Catalog No.: PC-44705Not For Human Use, Lab Use Only.

ONO-4059 (Tirabrutinib) hydrochloride is potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.

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

Biological Activity

ONO-4059 (Tirabrutinib) hydrochloride is potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.
ONO-4059 (Tirabrutinib) shows weak activity against wt EGFR (IC50=184 nM).
ONO-4059 (Tirabrutinib) inhibits signaling pathways and cellular growth in both EGFRm(+) and EGFRm(+)/T790M(+) mutant cell lines in vitro.
ONO-4059 (Tirabrutinib) exhibits tumor regression in EGFR-mutant tumor xenograft and transgenic models; orally active.

Physicochemical Properties

M.Wt 490.9415
Formula C25H23ClN6O3
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

10 mM in DMSO

Chemical Name/SMILES

8H-Purin-8-one, 6-amino-7,9-dihydro-9-[(3R)-1-(1-oxo-2-butyn-1-yl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-, hydrochloride (1:1)

References

1. Walter HS, et al. Blood. 2016 Jan 28;127(4):411-9.

2. Yahiaoui A, et al. PLoS One. 2017 Feb 8;12(2):e0171221.

3. Yasuhiro T, et al. Leuk Lymphoma. 2017 Mar;58(3):699-707.

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