ONO-4059 is a selective and novel inhibitor of BTK with IC50 2.2 nm, ONO-4059 binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. BTK is potently inhibited by ONO/GS-4059 with a 50% inhibitory concentration of 2 nmol/L. ONO -4059 induces classical apoptosis at nanomolar concentrations in the activated B-cell diffuse large B-cell lymphoma (DLBCL) cell line, TMD-822 and in a TMD-8 xenograft model, treatment with ONO -4059 resulted in inhibition of tumor growth.
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名称 | Tirabrutinib HCl |
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Iupac 化学名称 | (R)-6-amino-9-(1-(but-2-ynoyl)pyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride |
同义词 | ONO-4059 HCl ; ONO4059 ; ONO 4059 ; ONO-4059 ; GS 4059 ; GS-4059 ; GS4059 ; ONO-WG-307 ; Tirabrutinib |
英文同义词 | ONO-4059 HCl ; ONO4059 ; ONO 4059 ; ONO-4059 ; GS 4059 ; GS-4059 ; GS4059 ; ONO-WG-307 ; Tirabrutinib |
分子式 | C₂₅H₂₃ClN₆O₃ |
分子量 | 490.94 |
Smile | O=C1N(C2=CC=C(OC3=CC=CC=C3)C=C2)C4=C(N)N=CN=C4N1[C@H]5CN(C(C#CC)=O)CC5.[H]Cl |
InChiKey | UQYDCIJFACDXSG-GMUIIQOCSA-N |
InChi | InChI=1S/C25H22N6O3.ClH/c1-2-6-21(32)29-14-13-18(15-29)31-24-22(23(26)27-16-28-24)30(25(31)33)17-9-11-20(12-10-17)34-19-7-4-3-5-8-19;/h3-5,7-12,16,18H,13-15H2,1H3,(H2,26,27,28);1H/t18-;/m1./s1 |
Cas号 | 1439901-97-9 |
相关CAS号 | 1439901-97-9 (HCl) 1351636-18-4 (free base) |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | Off-white solid to white solid |
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纯度 | ≧98.0% |
存储 | 3 years -20ºCpowder |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature as non-hazardous chemical. |
海关编码 |
Targets | BTK inhibitor |
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Mechanism | ONO-4059 is a selective and novel inhibitor of BTK with IC50 2.2 nm, ONO-4059 binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. |
Cell study | |
Animal study | |
Clinical study |