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Vodobatinib

Chemical Structure : Vodobatinib

CAS No.: 1388803-90-4

Vodobatinib (K0706, K 0706)

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).

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Biological Activity

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.

Physicochemical Properties

M.Wt 453.926
Formula C27H20ClN3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-chloro-6-methyl-N'-(4-methyl-3-(quinolin-3-ylethynyl)benzoyl)benzohydrazide

References

1. Antelope O, et al. Exp Hematol. 2019 Sep;77:36-40.e2.

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