Orelabrutinib (Synonyms: ICP-022)
目录号: PL03044 纯度: ≥99%
CAS No. :1655504-04-3
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中文名称
Orelabrutinib
英文名称
Orelabrutinib
英文别名
Orelabrutinib;6-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)nicotinamide;WJA5UO9E10;orelabrutinib (proposed INN);ICP022;US9951056, Example 3;GTPL10629;MZPVEMOYADUARK-UHFFFAOYSA-N;BDBM389631;example 3 [WO2015048662A2];ICP-022
Cas No.
1655504-04-3
分子式
C26H25N3O3
分子量
427.50
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Orelabrutinib (ICP-022) 是一种强效、口服活性、不可逆的 Bruton 酪氨酸激酶 (BTK) 抑制剂,具有潜在的抗肿瘤活性。Orelabrutinib 可阻止 B 细胞抗原受体 (BCR) 信号通路的激活和 BTK 介导的下游生存通路的激活,抑制过度表达 BTK 的恶性 B 细胞的生长。
生物活性
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Brutons tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
性状
Solid
体外研究(In Vitro)
With a proprietary formulation, Orelabrutinib (ICP-022) achieves high bioavailability comparing to other BTK inhibitors. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Upon administration, Orelabrutinib (ICP-022) binds to and inhibits the activity of BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK. 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]. Wei Xu, et al. Safety, Tolerability and Efficacy of Orelabrutinib, Once a Day, to Treat Chinese Patients with Relapsed or Refractory Chronic Lymphocytic Leukemia/Small Cell Leukemia. Blood (2019) 134 (Supplement_1): 4319.
[2]. BTK Inhibitor ICP-022.
溶解度数据
In Vitro: DMSO : 100 mg/mL (233.92 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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