Catalog No.: PC-38379Not For Human Use, Lab Use Only.
Vodobatinib (K0706) is a potent, selective inhibitor of BCR-ABL1 with IC50 of 7 nM (wt BCR-ABL1), exhibits activity against most clinically important BCR-ABL1 point mutants (M244V, IC50=22 nM).
Vodobatinib (K0706) is a potent, selective inhibitor of BCR-ABL1 with IC50 of 7 nM (wt BCR-ABL1), exhibits activity against most clinically important BCR-ABL1 point mutants (M244V, IC50=22 nM).
The only BCR-ABL1 point mutants with IC50 above 100 nM are: BCR-ABL1L248R (IC50: 167 nM), BCR-ABL1Y253H (IC50: 154 nM), BCR-ABL1E255V (IC50: 165 nM) and BCR-ABL1T315I (IC50: 1967 nM).
Vodobatinib (K0706) demonstrated direct, potent inhibition of BCR-ABL1 tyrosine autophosphorylation as well as inhibition of BCR-ABL1L248R, BCR-ABL1Y253H and BCR-ABL1E255V at high concentrations in a panel of cell lines expressing TKI resistant mutants of BCR-ABL1.
Vodobatinib (K0706) does not inhibit mutant BCR-ABL1T315I.
Vodobatinib (K0706) exhibited pre-clinical activity in Philadelphia chromosome-positive leukemia.
