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Asciminib (ABL001) selectively inhibited the growth of CML and Ph+ ALL cells with potencies ranging from 1-10nM range. Asciminib was tested for activity against clinically observed mutations and found to be active in the low nM range. In the KCL-22 mouse xenograft model, Asciminib displayed potent anti-tumor activity with complete tumor regression observed and a clear dose-dependent correlation with pSTAT5 inhibition. The oral bioavailability of ABL001 in mouse and rat are 35% and 27% respectively when dosed at 30 mg/kg p.o. While in dogs the oral BA of ABL001 is 111% (15 mg/kg, p.o).
| Molecular Weight | 449.84 |
| Formula | C20H18ClF2N5O3 |
| CAS Number | 1492952-76-7 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Wylie AA, et al. Nature. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.
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