1433820-83-7
1433820-83-7 structure
- Name: GNE-431
- Chemical Name: GNE-431
- CAS Number: 1433820-83-7
- Molecular Formula: C30H32N10O2
- Molecular Weight: 564.654
- Create Date: 2020-01-11 16:06:50
- Modify Date: 2024-04-12 12:01:40
-
GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively; shows higher selectivity for Btk than any of the covalent inhibitors or non-covalent analogs profiled; does not interact with Cys481 and differs from covalent inhibitors like ibrutinib, potently inhibits the ibrutinib-resistant Btk C481S mutant in vitro and in cells; also shows excellent potency against the C481R, T474I, and T474M mutants (IC50=7.5-10 nM); potently inhibits BCR signaling in stimulated human blood and blocks Btk autophosphorylation in C481S-transfected cells.
| Name | GNE-431 |
|---|
| Description | GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively; shows higher selectivity for Btk than any of the covalent inhibitors or non-covalent analogs profiled; does not interact with Cys481 and differs from covalent inhibitors like ibrutinib, potently inhibits the ibrutinib-resistant Btk C481S mutant in vitro and in cells; also shows excellent potency against the C481R, T474I, and T474M mutants (IC50=7.5-10 nM); potently inhibits BCR signaling in stimulated human blood and blocks Btk autophosphorylation in C481S-transfected cells. |
|---|---|
| References | References 1. Johnson AR, et al. ACS Chem Biol. 2016 Oct 21;11(10):2897-2907. View Related Products by Target BTK |
| Molecular Formula | C30H32N10O2 |
|---|---|
| Molecular Weight | 564.654 |