Tirabrutinib hydrochloride|1439901-97-9|(ONO-4059 hydrochloride; GS-4059 hydrochloride)-陌孚医药/Medlife

您当前的位置：

Tirabrutinib hydrochloride (Synonyms: ONO-4059 hydrochloride; GS-4059 hydrochloride)

目录号: PL04529 纯度: ≥99%

CAS No. :1439901-97-9

商品编号	规格	价格	会员价
PL04529-5mg	5mg	¥964.00	请登录
PL04529-10mg	10mg	¥1607.00	请登录
PL04529-25mg	25mg	¥3214.00	请登录
PL04529-50mg	50mg	¥5625.00	请登录
PL04529-100mg	100mg	¥9643.00	请登录
PL04529-200mg	200mg	询价	询价
PL04529-500mg	500mg	询价	询价
PL04529-10mM*1mLinDMSO	10mM*1mLinDMSO	¥1060.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称	Tirabrutinib hydrochloride
中文别名	ONO-4059 (hydrochloride)
英文名称	Tirabrutinib hydrochloride
英文别名	(R)-6-amino-9-(1-but-2-ynoylpyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one;ONO-4059 (GS-4059) hydrochloride;ONO-4059 (HYDROCHLORIDE);GS4059 hydrochloride;GS-4059 hydrochloride;ONO4059 hydrochloride;ONO-4059(HCl salt);Tirabrutinib hydrochloride
Cas No.	1439901-97-9
分子式	C₂₅H₂₂N₆O₃^.HCl
分子量	490.94
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Tirabrutinib (ONO-4059) hydrochloride 是一种口服有效的高选择性 Bruton’s Tyrosine Kinase (BTK) 抑制剂 (能透过血脑屏障)，其 IC₅₀ 值为 6.8 nM。Tirabrutinib hydrochloride 不可逆共价结合 BTK 并抑制异常 B 细胞受体信号传导。Tirabrutinib hydrochloride 可用于自身免疫性疾病和血液学恶性肿瘤的研究。

生物活性

Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC 50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies.

性状

Solid

IC50 & Target[1][2]

BMX 6 nM (IC50) BTK 6.8 nM (IC50

体外研究(In Vitro)

Tirabrutinib hydrochloride (0.1-1000 nM or 0.001-100 nM; 72 h) inhibits the proliferation of OCI-L Y10 and SU-DHL-6 cells with IC50s of 9.127 nM, and 17.10 nM, respectively.
Tirabrutinib hydrochloride (0.5, 5, 50 μM; 24, 48 h) induces SU-DHL-6 cells apoptosis needs high dosage and prolonged administration (concentration up to 50 μM and incubates for 48 h).
Tirabrutinib hydrochloride (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Tirabrutinib hydrochloride (10 mg/kg; p.o.; single) is rapidly absorbed into plasma and brain, and reaches C max (blood C max =339.53 ng/mL; brain C max =28.9 ng/mL) 2 hours post administration.
Tirabrutinib hydrochloride (6, 20 mg/kg; p.o.; single daily for 3 weeks) shows inhibition of tumour growth in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Yu H, et al. Brutons tyrosine kinase inhibitors in primary central nervous system lymphoma-evaluation of anti-tumor efficacy and brain distribution. Transl Cancer Res. 2021 May;10(5):1975-1983.
[2]. Kozaki R, et al. Responses to the Selective Brutons Tyrosine Kinase (BTK) Inhibitor Tirabrutinib (ONO/GS-4059) in Diffuse Large B-cell Lymphoma Cell Lines. Cancers (Basel). 2018 Apr 23;10(4):127.

溶解度数据	In Vitro: DMSO : 100 mg/mL (203.69 mM; Need ultrasonic)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation