Molecular Formula | C22H22FN5O3 |
Molar Mass | 423.44 |
Density | 1.322±0.06 g/cm3(Predicted) |
Solubility | DMSO 85 mg/mL (200.73 mM);Water <1 mg/mL (<1 mM);Ethanol <1 mg/mL (<1 mM) |
pKa | 13.22±0.70(Predicted) |
Storage Condition | -20℃ |
MDL | MFCD25976876 |
In vitro study | AVL-292 produced a dose-dependent inhibition of BTK in Ramos cells with an EC50 of 8 nM; And inhibited the downstream BCR pathway. AVL-292 by inhibiting the activity of BTK, the proliferation of B cells was further inhibited, and the EC50 was 3 nM. |
In vivo study | In the collagen-induced mouse arthritis model, AVL-292 (3- 30 mg/kg, p.o.) dose-dependent suppression of the clinical symptoms of such inflammation, including swelling of the joints and paws and a reduction in symptoms of redness of the affected paw. |
introduction | AVL-292 is a BTK inhibitor that can be used orally through covalent bai binding and has a highly selective du. its IC50 is less than zhi0.5 nM, showing that dao is at least 1400 times more selective than other tested kinases. |
application | AVL-292 is an effective inhibitor of Btk kinase activity, which can be used in laboratory scientific research. |
effect | AVL-292 produced a dose-dependent inhibition of BTK in Ramos cells with an EC50 of 8 nM; And inhibited the downstream BCR pathway. AVL-292 further inhibited the proliferation of B cells by inhibiting the activity of BTK, and its EC50 was 3 nM. In the collagen-induced mouse arthritis model, AVL-292 (3- 30 mg/kg, p.o.) dose-dependently inhibited the clinical symptoms of such inflammation, including swelling of joints and claws and the reduction of red symptoms of affected claws. |
biological activity | Spebrutinib (CC-292, AVL-292) is a highly selective BTK inhibitor that is covalently bound and can be taken orally. Its IC50 is less than 0.5 nM, showing at least 1400 times selectivity than other tested kinases. Phase 1. |
target | TargetValue BTK (Cell-free assay) <0.5 nM |
Target | Value |
BTK (Cell-free assay) | <0.5 nM |
in vitro study | AVL-292 produced dose-dependent inhibition of BTK in Ramos cells, with EC50 of 8 nM; And inhibited the downstream BCR pathway. AVL-292 further inhibited the proliferation of B cells by inhibiting the activity of BTK, and its EC50 was 3 nM. |
in vivo study | in collagen-induced mouse arthritis model, AVL-292 (3-30mg/kg, p.o.) dose-dependently inhibited the clinical symptoms of such inflammation, including the swelling of joints and claws and the reduction of red symptoms of affected claws. |