Shopping Cart
- Remove All
- Your shopping cart is currently empty
Vecabrutinib (SNS-062) is a potent, noncovalent inhibitor of BTK (Kd: 0.3 nM) and ITK (Kd: 2.2 nM), with an IC50 of 24 nM for ITK.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $79 | In Stock | |
5 mg | $196 | In Stock | |
10 mg | $322 | In Stock | |
25 mg | $523 | In Stock | |
50 mg | $693 | In Stock | |
100 mg | $972 | In Stock | |
1 mL x 10 mM (in DMSO) | $231 | In Stock |
Description | Vecabrutinib (SNS-062) is a potent, noncovalent inhibitor of BTK (Kd: 0.3 nM) and ITK (Kd: 2.2 nM), with an IC50 of 24 nM for ITK. |
Targets&IC50 | ITK:2.2 nM(kd), ITK:24 nM, BTK:(kd)0.3 nM |
In vitro | Vecabrutinib is six times more potent than PCI-32765 and greater than 640 times more potent than acalabrutinib against C481S BTK. Vecabrutinib inhibits pBTK in human whole blood (average IC50: 50 nM). Vecabrutinib inhibits WT and C481S BTK with similar IC50s (pBTK IC50s: 2.9 nM and 4.4 nM for WT BTK and C481S BTK). In a recombinant kinase assay, IC50s of Vecabrutinib against WT BTK and C481S BTK are 4.6 nM and 1.1 nM. Vecabrutinib retains activity against the mutated BTK variant. Vecabrutinib demonstrates dose-dependent inhibition of BTK in primary patient CLL cells comparable to PCI-32765 via immunoblot for BTK phosphorylation. Vecabrutinib decreases the viability of primary CLL cells in the presence of HS5 stromal protection by 5.5% [1][2]. |
In vivo | Vecabrutinib is well tolerated with continuous drug levels. Vecabrutinib has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours [1]. |
Alias | SNS-062 |
Molecular Weight | 529.92 |
Formula | C22H24ClF4N7O2 |
Cas No. | 1510829-06-7 |
Smiles | NC(=O)[C@H]1CCN(C[C@@H]1N1CCC[C@@H](Nc2cc(Cl)cc(c2)C(F)(F)F)C1=O)c1ncnc(N)c1F |
Relative Density. | 1.509 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 112.5 mg/mL (212.3 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.