- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S2680||Ibrutinib (PCI-32765)||<1 mg/mL||88 mg/mL||45 mg/mL|
|S7173||CC-292 (AVL-292)||<1 mg/mL||85 mg/mL||<1 mg/mL|
|S7257||CNX-774||<1 mg/mL||100 mg/mL||2 mg/mL|
|S7080||RN486||<1 mg/mL||62 mg/mL||<1 mg/mL|
|S7734||LFM-A13||<1 mg/mL||72 mg/mL||<1 mg/mL|
|S8166||ONO-4059 (GS-4059) hydrochloride||<1 mg/mL||98 mg/mL||1 mg/mL|
|S7877||ONO-4059 analogue||<1 mg/mL||20 mg/mL||<1 mg/mL|
|S8116||Acalabrutinib (ACP-196)||<1 mg/mL||93 mg/mL||93 mg/mL|
|S7051||CGI1746||<1 mg/mL||100 mg/mL||33 mg/mL|
- BTK Inhibitors (9)
- New BTK Products
|Catalog No.||Information||Product Use Citations||Product Validations|
Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.
BTK C481S and C481T variants show resistance to ibrutinib. (a and b) COS-7 cells were transfected with wild-type BTK or the two variants. Thirty-six hours post transfection, the cells were serum starved and treated with ibrutinib overnight followed by activation with serum and pervanadate for 5 min at room temperature. The cell lysates were immunoblotted for pY223 BTK and pY753 PLCγ2.
CC-292 (AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1.
Effects of AVL-292, CNX-774 and dasatinib on IgE-mediated histamine release in human basophils. Basophils (BA) obtained from three nonallergic donors (A).
CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.
Effects of AVL-292, CNX-774 and dasatinib on IgE-mediated histamine release in human basophils. Basophils (BA) obtained from three nonallergic donors (A), three patients allergic to Der p 2, and three patients allergic to Phl p 5 (B and C) were preincubated in control medium (Co) or medium containing various concentrations of AVL-292, CNX-774, or dasatinib (0.001-1 μmol/L) at 37°C for 30 minutes. Then, cells were exposed to anti-IgE antibody E-124.2.8 (1 μg/mL; nonallergic donors) or recombinant allergens (1 μg/mL of rDer p 2 or rPhl p 5 in allergic patients) at 37°C for 30 minutes. After centrifugation, histamine concentrations were determined in cell-free supernatants and cell lysates. Histamine release is expressed as percentage of total histamine. Results show the percentage of control and represent mean SD from three independent experiments (three donors). Asterisk (*): P<0.05 by Student's t test with Bonferroni correction
RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.
LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK.
Crosslinking FcγRIIB triggers apoptosis through Btk and p38 MAPK in human B cells. a Purified naïve, memory B cells and PCs (105/ml) from seven donors were each treated with 10 μg/ml of ICs in the presence of either 2 μM of LFM-A13 or 10 nM of ibrutinib for 24 h. Apoptotic cells were determined by Annexin V staining (Biolegend) using flow cytometry. The asterisks indicate that the differences between the groups compared are statistically significant (P < 0.05).
ONO-4059 (GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.
ONO-4059 analogue is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1.
Acalabrutinib(ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR.
CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.