切换导航

AVL-292

现货
Catalog No.
A3206
Btk抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 880.00
现货
10mg
¥ 1,200.00
现货
50mg
¥ 3,500.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

CC-292, formerly known as AVL-292, is an orally active, potent irreversible small molecule inhibitor of BTK with IC50 of 0.5 nM and EC50 of 8 nM. [1]
The B cell receptor (BCR) signaling pathway plays an important role in the fate and function of B cells by modulating cellular selection, maturation, proliferation, and production of antibody.
BTK, which is a tyrosine kinase member of the Tec kinase family, is a unique therapeutic target among kinases in the pathway BCR signaling. Studies showed that loss of gene function mutations of BTK in humans consequently leads to X-linked agammaglobulinaemia (XLA), characterized by a complete lack of B cells, low concentrations of serum Ig, and recurring infections, which implies that BTK is required in the development and immunoglobulin production of B cells. CC-292 inhibits BTK by the formation of a covalent bond with Cys481 residue. [2]
The inhibitory activity of CC-292 has been examined in immunoblot analysis, which showed that CC-292 potently inhibits auto-phosphorylation in human naive primary B cells. Furthermore, CD69 upregulation tested by flow cytometry tracking also exhibited a dose-dependent reduction in CD69 expression with increasing levels of CC-292 in vitro. Covalent probe analysis of human B cells coupled with enzyme linked immunosorbent assay (ELISA) quantification methods illustrated 42% BTK occupancy in a 1h incubation with CC-292 of 10 nM. [1, 2]
Studies in vivo for CC-292 has been conducted. CIA model in mice was orally treated with CC-292, which demonstrated a positive correlation between BTK occupancy and inhibition of the disease. In addition, CC-292 was assessed with clinical trials, which showed a T1/2 of 1.9h and suggested efficacy in B-NHL, WM, and CLL patients. [2]
References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt423.44
Cas No.1202757-89-8
FormulaC22H22FN5O3
SynonymsAVL292;AVL 292
Solubility≥21.15 mg/mL in DMSO, ≥4.9 mg/mL in EtOH with ultrasonic and warming, <2.23 mg/mL in H2O
Chemical NameN-[3-[[5-fluoro-2-[4-(2-methoxyethoxy)anilino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide
SDFDownload SDF
Canonical SMILESCOCCOC1=CC=C(C=C1)NC2=NC=C(C(=N2)NC3=CC(=CC=C3)NC(=O)C=C)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。

生物活性

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

化学结构

AVL-292