Tirabrutinib (ONO-4059, GS-4059) | mutant EGFR inhibitor

Chemical Structure : Tirabrutinib

CAS No.: 1351636-18-4

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Tirabrutinib (ONO4059, ONO-4059, GS4059)

货号: 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.

规格	价格	库存
10 mg	￥880	In stock
25 mg	￥1480	In stock
50 mg	￥2380	In stock
100 mg	￥3880	In stock
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	454.4806
分子式	C25H22N6O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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)-

参考文献

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.

Tirabrutinib (ONO4059, ONO-4059, GS4059)

生物&药学活性

物理化学性质&存储条件

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Tirabrutinib (ONO4059, ONO-4059, GS4059)

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物理化学性质&存储条件

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