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Chemical Structure : Tirabrutinib
CAS No.: 1351636-18-4
Catalog No.: PC-44704Not For Human Use, Lab Use Only.
Tirabrutinib (ONO 4059, GS 4059) is a potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $98 | In stock | |
| 25 mg | $158 | In stock | |
| 50 mg | $248 | In stock | |
| 100 mg | Get quote |
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Tirabrutinib (ONO 4059, GS 4059) is a potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.
Tirabrutinib (ONO 4059, GS 4059) shows weak activity against wt EGFR (IC50=184 nM).
Tirabrutinib (ONO 4059, GS 4059) inhibits signaling pathways and cellular growth in both EGFRm(+) and EGFRm(+)/T790M(+) mutant cell lines in vitro.
Tirabrutinib (ONO 4059, GS 4059) exhibits tumor regression in EGFR-mutant tumor xenograft and transgenic models; orally active.
| M.Wt | 454.4806 | |
| Formula | C25H22N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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)- |
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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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