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| 商品编号 | 规格 | 价格 | 会员价 | 是否有货 | 数量 |
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| PL04529-5mg | 5mg | ¥474.00 | 请登录 |
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| PL04529-10mg | 10mg | ¥823.00 | 请登录 |
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| PL04529-25mg | 25mg | ¥1645.00 | 请登录 |
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| PL04529-50mg | 50mg | ¥2475.00 | 请登录 |
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| PL04529-100mg | 100mg | ¥3725.00 | 请登录 |
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| PL04529-200mg | 200mg | 询价 | 询价 |
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| PL04529-500mg | 500mg | 询价 | 询价 |
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| PL04529-10mM*1mLinDMSO | 10mM*1mLinDMSO | ¥1060.00 | 请登录 |
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| PL04529-1 mL x 10 mM (in DMSO) | ¥541.00 | 请登录 |
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| 中文名称 |
Tirabrutinib hydrochloride
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|---|---|
| 中文别名 |
ONO-4059 (hydrochloride)
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| 英文名称 |
Tirabrutinib hydrochloride
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| 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
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| Cas No. |
1439901-97-9
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| 分子式 |
C25H22N6O3.HCl
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| 分子量 |
490.94
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| 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)
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| 详情描述 |
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。
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| 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。
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|---|---|
| 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.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
BMX 6 nM (IC50) BTK 6.8 nM (IC50
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| 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.
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| 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.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 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)
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| ClinicalTrial |
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| 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.
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| 溶解度数据 |
In Vitro: DMSO : 100 mg/mL (203.69 mM; Need ultrasonic)配制储备液
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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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