ONO-4059 (HYDROCHLORIDE)
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- CAS号:
- 1439901-97-9
- 英文名:
- ONO-4059 (hydrochloride)
- 英文别名:
- ON 0459;ON-0459;ONO-WG-307;ONO-4059 HCl;ON 0459;ON-0459;Tirabrutinib HCl;ONO-4059(HCl salt);ONO-4059 (GS-4059);GS-4059 (hydrochloride);ONO-4059 (hydrochloride)
- 中文名:
- ONO-4059 (HYDROCHLORIDE)
- 中文别名:
- 替拉鲁替尼 盐酸盐;TIRABRUTINIB 盐酸盐;盐酸替拉鲁替尼(ONO-4059);化合物TIRABRUTINIB HYDROCHLORIDE;B细胞受体抑制剂(ONO-4059 HYDROCHLORIDE);(R) -6-氨基-9-(1-(丁-2-炔酰基)吡咯烷-3-基)-7-(4-苯氧基苯基)-7,9-二氢-8H-嘌呤-8-酮盐酸盐
- CBNumber:
- CB93126702
- 分子式:
- C25H23ClN6O3
- 分子量:
- 490.95
- MOL File:
- 1439901-97-9.mol
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ONO-4059 (HYDROCHLORIDE)化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMF: 1 mg/ml; DMSO: 1 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
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形态:
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A crystalline solid
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颜色:
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White to off-white
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ONO-4059 (HYDROCHLORIDE)性质、用途与生产工艺
Tirabrutinib Hydrochloride (ONO-4059, GS-4059) 是一种高度有效的、选择性的BTK抑制剂,IC50为2.2 nM。
相较于Lck、 Fyn、LynA,ONO-4059对BTK的选择性更大,并只以浓度依赖性方式抑制anti-IgM诱导的B细胞激活,而不抑制anti-CD3/CD28诱导的人类PBMCs向T淋巴细胞的激活。ONO/GS-4059在一些恶性B细胞中抑制细胞增殖,但也在纳摩尔浓度范围内,诱导TMD8细胞的经典凋亡反应。
在CIA小鼠模型中,ONO-4059通过抑制炎性趋化因子和单核细胞中细胞因子如IL-6、IL-8、TNFalpha等的产生,发挥疗效,同时伴随软骨侵蚀、骨损伤、血管翳形成的消退。在临床前动物模型和临床CLL、NHL患者中,ONO-4059具有抗肿瘤活性,安全性良好,药效长久。
用途
一种有效的口服活性的BTK(布鲁顿酪氨酸激酶)抑制剂, IC50:2.2nM。Tirabrutinib HCl is a potent and orally active Bruton agammaglobulinemia tyrosine kinase (BTK) in hibitor. Upon administration, ONO-4059 covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.
ONO-4059 (HYDROCHLORIDE)
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/08/19 | HY-15771A | Tirabrutinib hydrochloride | | 1 mg | 240元 |
2024/08/19 | HY-15771A | ONO-4059 (HYDROCHLORIDE) Tirabrutinib hydrochloride | 1439901-97-9 | 5mg | 600元 |
ONO-4059 (HYDROCHLORIDE)
生产厂家
1439901-97-9, ONO-4059 (HYDROCHLORIDE) 相关搜索:
- 抑制剂
- 药靶配体
- 细胞生物学试剂
- 盐酸替拉鲁替尼(ONO-4059)
- TIRABRUTINIB 盐酸盐
- 化合物TIRABRUTINIB HYDROCHLORIDE
- (R) -6-氨基-9-(1-(丁-2-炔酰基)吡咯烷-3-基)-7-(4-苯氧基苯基)-7,9-二氢-8H-嘌呤-8-酮盐酸盐
- B细胞受体抑制剂(ONO-4059 HYDROCHLORIDE)
- 替拉鲁替尼 盐酸盐
- 1439901-97-9
- ONO-4059 (GS-4059)
- B cells,GS-4059,haematological malignancies,Bruton tyrosine kinase,GS4059,PCNSL,Tirabrutinib,ONO4059,GS 4059,ONO 4059,Inhibitor,ONO-4059,autoimmune disorders,Tirabrutinib hydrochloride,Apoptosis,Btk,inhibit
- tirabrutinib(GS-4059/ONO-4059) hydrochloride
- Tirabrutinib (ONO-4059) HCl
- ONO-WG-307
- ONO-4059 HCL; ONO4059; ONO 4059; ONO-4059; GS 4059; GS-4059; GS4059; ONO-WG-307; TIRABRUTINIB
- Tirabrutinib HCl
- TIRABRUTINIB HYDROCHLORIDE;GS-4059 (HYDROCHLORIDE)
- Tirabrutinib hydrochloride
- GS-4059 (hydrochloride)
- TIRABRUTINIB (ONO-4059) HYDROCHLORIDE
- ON-0459
- ON 0459;ON-0459
- ON 0459
- ONO-4059(HCl salt)
- (R)-6-amino-9-(1-but-2-ynoylpyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one HCl salt
- (R)-6-amino-9-(1-(but-2-ynoyl)pyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride
- ONO-4059 HCl
- ONO-4059(GS4059) hydrochloride
- (R)-6-amino-9-(1-but-2-ynoylpyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one
- ONO-4059 (hydrochloride)