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Chemical Structure : NVP-CLR457
Catalog No.: PC-38635Not For Human Use, Lab Use Only.
NVP-CLR457 (CLR457) is a potent, orally bioavailable, non-CNS-penetrant pan-class I PI3K inhibitor with IC50 values of 89 nM, 56 nM, 39 nM and 230 nM for p110α, p110β, p110δ and p110γ isoforms, respectively.
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NVP-CLR457 (CLR457) is a potent, orally bioavailable, non-CNS-penetrant pan-class I PI3K inhibitor with IC50 values of 89 nM, 56 nM, 39 nM and 230 nM for p110α, p110β, p110δ and p110γ isoforms, respectively.
NVP-CLR457 (CLR457) also inhibited the most common forms of PIK3CA mutant isoforms: E545K (helical domain mutation) and H1047R (kinase domain mutation).
NVP-CLR457 (CLR457) demonstrated antitumor activity in multiple tumor xenograft models with constitutively active PI3K pathway.
| M.Wt | 455.398 | |
| Formula | C18H20F3N7O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. James J Harding, et al. Invest New Drugs. 2019 Apr;37(2):271-281.
2. Robin A Fairhurst, et al. J Med Chem. 2022 May 2. doi: 10.1021/acs.jmedchem.2c00267.
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