Tirabrutinib
产品说明书
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同义名 : | ONO-4059; GS-4059; ONO-WG-307 |
| CAS号 : | 1351636-18-4 | |
| 货号 : | A146088 | |
| 分子式 : | C25H22N6O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 454.48 | |
| MDL号 : | MFCD28386296 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | BTK (Bruton Tyrosine Kinase) is a cytoplasmic, non-receptor tyrosine kinase that transmits signals from a variety of cell-surface molecules, including the B-cell receptor (BCR) and tissue homing receptors. BTK is indispensable for B lymphocyte development, differentiation and signaling, and plays a crucial role in B-cell development[3]. ONO-4059 is a BTK inhibitor. The IC50 of ONO-4059 against BTK kinase was 2.2 nM[3]. ONO-4059 inhibited the TMD-8 cell growth with the IC50 of 3.59 nM for 72h as determined by a cell viability assay. ONO-4059 also concentration-dependently inhibited BTK phosphorylation with the IC50 of 23.9 nM for 4h[4]. In a TMD-8 xenograft model established in SCID mice, ONO-4059 was administered orally or mixed in food at doses up to 20 mg/kg/day and animals were dosed QD or BD. For the groups that treatment started when tumor volume was 100 - 200mm3, tumor growth inhibition of ONO-4059 treated groups was 23% in QD, 72.9% in BD and 100% in dose mixed in food, respectively. For the groups that treatment started when tumor volume was 400 - 450mm3, no growth inhibition was observed in the QD group and growth inhibitions of 27.5% in BD and 100% in dose mixed in food were observed[5]. In another study of TMD-8 xenograft model, ONO-4059 was administered via mixed diet at an indicated relative content of 0.0037%. This dose resulted in tumor growth inhibition of 56.1% as a single agent and significantly enhanced the anti-tumor activity of Rituximab[6]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.20mL 0.44mL 0.22mL |
11.00mL 2.20mL 1.10mL |
22.00mL 4.40mL 2.20mL |
| 参考文献 |
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