China (Mainland)
Premiumsupplier 
AVL292 CAS NO.1202757-89-8
- FOB Price: USD: 1.00-1.00 /Gram Get Latest Price
- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
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
- ProName: AVL292
- CasNo: 1202757-89-8
- Molecular Formula: C22H22FN5O3
- Appearance: off white powder
- Application: CAS：1202757-89-8； AVL-292;LMK-435;N-[...
- DeliveryTime: 3 months
- PackAge: 100g,500g,1kg,25kg
- Port: shang hai
- ProductionCapacity: 1000 Metric Ton/Month
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
We are committed to provide excellence in researching, manufacturing and drug discovery process.
Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.
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.