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Tirabrutinib HCl

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Chemical Structure| 1439901-97-9 同义名 : GS-4059 hydrochloride;ONO-4059 hydrochloride;ONO-WG-307;ONO-4059 (hydrochloride);GS-4059;Tirabrutinib hydrochloride
CAS号 : 1439901-97-9
货号 : A169176
分子式 : C25H23ClN6O3
纯度 : 99%+
分子量 : 490.942
MDL号 : MFCD30187521
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(213.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Tirabrutinib hydrochloride, known as ONO-4059 hydrochloride, is an orally bioavailable inhibitor of Bruton’s Tyrosine Kinase (BTK) capable of crossing the blood-brain barrier (BBB), with an IC50 of 6.8 nM. It forms an irreversible and covalent bond with BTK, inhibiting abnormal B cell receptor signaling pathways. This property makes tirabrutinib hydrochloride applicable for research into autoimmune diseases and hematological cancers[1].[2].[3].[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.18mL

2.04mL

1.02mL

20.37mL

4.07mL

2.04mL
参考文献

[1]Yu H, et al. Bruton's 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 Bruton's Tyrosine Kinase (BTK) Inhibitor Tirabrutinib (ONO/GS-4059) in Diffuse Large B-cell Lymphoma Cell Lines. Cancers (Basel). 2018 Apr 23;10(4):127.

[3]Liclican A, et al. Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition. Biochim Biophys Acta Gen Subj. 2020 Apr;1864(4):129531.

[4]Dhillon S. Tirabrutinib: First Approval. Drugs. 2020 Jun;80(8):835-840.