Chemical Structure : Zinilisib
CAS No.:
3031974-57-6
Zinilisib
(OKI-219, OKI 219)
Catalog No.: PC-28524Not For Human Use, Lab Use Only.
Zinilisib (OKI-219) is a potent, highly mutant-selective, brain penetrant and orally bioavailable inhibitor of PI3kα H1047 mutant, 100-fold selectivity for PI3KαH1047R over PI3KαWT.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Zinilisib (OKI-219) is a potent, highly mutant-selective, brain penetrant and orally bioavailable inhibitor of PI3kα H1047 mutant, 100-fold selectivity for PI3KαH1047R over PI3KαWT.
OKI-219 drives decreased phosphorylated AKT (pAKT) and decreased proliferation selectively in PI3KαH1047R mutant cell lines across several tumor types.
OKI-219 is active as a single agent in breast tumor models that have the PI3KαH1047R mutation.
OKI-219 is highly active in preclinical models of PI3KαH1047R-mutated cancer, including models of CNS disease, without the toxicities associated with wild-type inhibition.
Physicochemical Properties
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M.Wt
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502.54
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Formula
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C26H29F3N4O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-2-((1-(2,7-dimethyl-1-oxo-3-(4-(2,2,2-trifluoroethyl)piperazin-1-yl)-1,2-dihydroisoquinolin-5-yl)ethyl)amino)benzoic acid
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References
1. Molly A Taylor, et al. Mol Cancer Ther (2023) 22 (12_Supplement): B163.
2. James F, et al. WO2024054469A1. WIPO (PCT). 2023-09-06.
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