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AVL-292 Btk inhibitor

Catalog No.A3206
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10mM (in 1mL DMSO)
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Sample solution is provided at 25 µL, 10mM.

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Chemical structure


Biological Activity

Description AVL-292 is a highly selective, orally active small-molecule inhibitor of Btk with IC50 value of 0.5 nM.
Targets Btk          
IC50 0.5 nM          

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Chemical Properties

Cas No. 1202757-89-8 SDF Download SDF
Synonyms AVL292;AVL 292
Chemical Name N-[3-[[5-fluoro-2-[4-(2-methoxyethoxy)anilino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide
Formula C22H22FN5O3 M.Wt 423.44
Solubility ≥21.15 mg/mL in DMSO, ≥4.9 mg/mL in EtOH with ultrasonic and warming, <2.23 mg/mL in H2O Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.


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]
[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.