Tirabrutinib|1351636-18-4|(ONO-4059; GS-4059)-陌孚医药/Medlife

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

目录号: PL04528 纯度: ≥99%

CAS No. :1351636-18-4

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中文名称	Tirabrutinib
中文别名	ONO-4059
英文名称	Tirabrutinib
英文别名	ONO-4059;GS4059;GS-4059;ONO4059;6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one;ONO 4059;6-Amino-9-(1-(but-2-ynoyl)pyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one;BCP18777;AK547263;AK171748;6-Amino9[1(but-2-ynoyl)pyrrolidin-3-yl]7(4-phenoxyphenyl)8,9-dihydro-7H-purin-8-one;6-amino-9-[(3R)-1-but-2-ynoylpyrrolidin-3-yl]-7-(4-phenoxyphenyl)purin-8-one;6-Amino-9-[1-(but-2-ynoyl)pyrrolidin-3-yl]-7-(4-phenoxyphenyl)-8,9-dihydro-7H-purin-8-one;8h-purin-8-one, 6-amino-7,9-dihydro-9-[1-(1-oxo-2-butyn-1-yl)-3-pyrrolidinyl;Tirabrutinib
Cas No.	1351636-18-4
分子式	C₂₅H₂₂N₆O₃
分子量	454.48
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Tirabrutinib (ONO-4059) 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 不可逆共价结合 BTK 并抑制异常 B 细胞受体信号传导。Tirabrutinib 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) 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 irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.

性状

Solid

体外研究(In Vitro)

Tirabrutinib (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 (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 (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 (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 (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

Powder -20°C 3 years；4°C 2 years

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 (220.03 mM)配制储备液

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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。

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