GNE-431

Research use only, not for human use.

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.

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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GNE431

Tyrosine Kinase

BTK

BTK

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1433820-83-7

564.654

C30H32N10O2

>98% (HPLC)

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O=C1N(C2=NC=CC(C3=NN4C=CN=C4C(NC(C=C5C6)=NN5CCN6C)=C3)=C2CO)CCN7C1=CC8=C7CCCC8

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

(-20℃)

With Ice Pack

≥ 2 years