| Cas No.: | 1433820-83-7 |
| Chemical Name: | 3,4,6,7,8,9-Hexahydro-2-[3-(hydroxymethyl)-4-[8-[(4,5,6,7-tetrahydro-5-methylpyrazolo[1,5-a]pyrazin-2-yl)amino]imidazo[1,2-b]pyridazin-6-yl]-2-pyridinyl]pyrazino[1,2-a]indol-1(2H)-one |
| Synonyms: | GNE431 |
| Formula: | C30H32N10O2 |
| M.Wt: | 564.654 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| 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. |

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