AVL-292
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CC-292(原名AVL-292)是一种口服有效的、高效的不可逆小分子BTK抑制剂,IC50值为0.5 nM,EC50值为8 nM[1]。
B细胞受体(BCR)信号通路通过调节细胞选择、成熟、增殖及抗体生成,在B细胞的命运与功能方面起着重要作用。作为Tec激酶家族中的一种酪氨酸激酶,BTK在BCR信号通路的激酶中是一个独特的治疗靶点。研究发现,人体内BTK基因功能缺失突变会导致X-连锁无丙种球蛋白血症(XLA),其特征为B细胞完全缺失、血清免疫球蛋白含量低及复发性感染,这些特征表明,在B细胞的发展和免疫球蛋白产生的过程中BTK不可缺少。CC-292通过与Cys481残基形成共价键来抑制BTK[2]。
已在免疫印迹分析中检验CC-292的抑制活性,其表明在人幼稚原代B细胞中,CC-292强效抑制自磷酸化。此外,经流式细胞术检测CD69的上调也表明,CD69表达呈剂量依赖性降低,且CC-292体外表达水平增加。人类B细胞共价探针分析及酶联免疫吸附试验(ELISA)量化方法表明,在浓度为10 nM的CC-292中孵育1小时后,BTK的占有率为42%。
进行CC-292体内研究,在胶原诱导性关节炎(CIA)小鼠模型中,CC-292口服给药,结果表明BTK占有率和疾病抑制性呈正相关关系。另外,临床试验评估CC-292,结果表明其半衰期为1.9小时,且对B-NHL、WM及CLL病人有疗效[2]。
参考文献:
[1]. Evans E K, Aslanian S, Karp R, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans[J]. Journal of Pharmacology and Experimental Therapeutics, 2013, 346(2): 219-228.
[2]. Aalipour A, Advani R H. Bruton tyrosine kinase inhibitors: a promising novel targeted treatment for B cell lymphomas[J]. British journal of haematology, 2013, 163(4): 436-443.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 423.44 |
Cas No. | 1202757-89-8 |
Formula | C22H22FN5O3 |
Synonyms | AVL292;AVL 292 |
Solubility | ≥21.15 mg/mL in DMSO; insoluble in H2O; ≥4.9 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | N-[3-[[5-fluoro-2-[4-(2-methoxyethoxy)anilino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide |
SDF | Download SDF |
Canonical SMILES | COCCOC1=CC=C(C=C1)NC2=NC=C(C(=N2)NC3=CC(=CC=C3)NC(=O)C=C)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | AVL-292是一种高选择性的、口服有效的小分子Btk抑制剂,IC50值为0.5 nM。 | |||||
靶点 | Btk | |||||
IC50 | 0.5 nM |
质量控制和MSDS
- 批次:
化学结构
![AVL-292](http://www.apexbt.com//media/diy/images/struct/A3206.png)