CasNo.1202757-89-8,AVL292,(1202757-89-8) Suppliers

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Keywords

AVL292 AVL-292;LMK-435;N-[3-[[5-Fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-2-propenamide;2-Propenamide, N-[3-[[5-fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-4-pyrimidinyl]amino]p 1202757-89-8

Quick Details

Appearance:off white powder
Application:CAS：1202757-89-8； AVL-292;LMK-435;N-[3-[[5-Fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-2-propenamide;2-Propenamide, N-[3-[[5-fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-
PackAge:100g,500g,1kg,25kg
ProductionCapacity:1000|Metric Ton|Month
Storage:Dry seal
Transportation:shipping

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Details:

AVL-292 is a covalent, highly selective, orally active small molecule inhibitor of Btk with IC50 value of 0.5 nM; >1400-fold selectivity over the other kinases assayed.
IC50 Value: < 0.5 nM [1]
in vitro: AVL-292 forms a covalent bond with Cys481 in Btk and potently inhibits Btk in biochemical (IC50 < 0.5nM) and cellular assays (EC50 1-10 nM) including -IgM stimulation of BCR signaling, B cell proliferation and activation. Ramos cells were treated with AVL-292 for 1 hour followed by stimulation of the BCR with 5 g/mL -IgM for 10 minutes on ice. Cell lysates were immunoblotted for Btk autophosphorylation (Y223), PLC2 phosphorylation as well as activation of downstream Erk signaling. AVL-292 inhibited Btk kinase activity in a cellular setting with EC50 between 1-10 nM [1].
in vivo: In healthy human subjects, AVL-292 was found to be safe and well tolerated following oral administration at dose levels ranging from 0.5-7.0 mg/kg. AVL-292 plasma levels and pharmacodynamic measurement of Btk engagement was dose-proportional across cohorts [1].
Subjects diagnosed with B cell malignancies received single daily oral doses of AVL-292 in continuous 28 day cycles. Total Btk content was determined in peripheral blood mononuclear cells at pre-dose, and Btk occupancy was determined 4 and 24 hours post dose on Day 1 and Day 28 [2].
Clinical trial: AVL-292 is currently being evaluated in a Phase 1b clinical trial in relapsed, refractory B cell malignancies including Chronic Lymphocytic Leukemia (CLL) and non-Hodgkin lymphomas.