NVP-CLR457 | class I PI3K inhibitor | Probechem Biochemicals

Chemical Structure : NVP-CLR457

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NVP-CLR457 (CLR457)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	455.398
分子式	C18H20F3N7O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(4S,5R)-3-(2'-amino-2-morpholino-4'-(trifluoromethyl)-[4,5'-bipyrimidin]-6-yl)-4-(hydroxymethyl)-5-methyloxazolidin-2-one

参考文献

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.

NVP-CLR457 (CLR457)

生物&药学活性

物理化学性质&存储条件

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NVP-CLR457 (CLR457)

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物理化学性质&存储条件

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