Chemical Structure : Zinilisib
货号: 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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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.
| 分子量 | 502.54 | |
| 分子式 | C26H29F3N4O3 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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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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