PERK inhibitor 28 | PERK inhibitor | Probechem Biochemicals

Chemical Structure : PERK inhibitor 28

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PERK inhibitor 28 (PERK-IN-5)

货号: PC-49644Not For Human Use, Lab Use Only.

PERK inhibitor 28 is a potent, selective, and orally bioavailable PERK inhibitor with biochemical IC50 of 2 nM, and cellular IC50 of 9 nM in p-eIF2α cellular TR-FRET assays.

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生物&药学活性

PERK inhibitor 28 is a potent, selective, and orally bioavailable PERK inhibitor with biochemical IC50 of 2 nM, and cellular IC50 of 9 nM in p-eIF2α cellular TR-FRET assays.
PERK inhibitor 28 shows a very clean kinase selectivity profile with S(35), S(10), and S(1) selectivity scores of 0.007, 0, and 0, respectively at a concentration of 1 μM in the 468-kinase scanMAXSM panel.
PERK inhibitor 28 (10 mg/kg BID) showed statistically significant tumor growth inhibition in the clear cell renal cell carcinoma (ccRCC)xenograft model 786-O.

物理化学性质&存储条件

分子量	468.50
分子式	C25H26F2N4O3
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	(R)-2-amino-5-(4-(2-(3,5-difluorophenyl)-2-hydroxyacetamido)-2-ethylphenyl)-N-isopropylnicotinamide

参考文献

1. Veronica Calvo, et al. Bioorg Med Chem Lett. 2021 Jul 1;43:128058.

PERK inhibitor 28 (PERK-IN-5)

生物&药学活性

物理化学性质&存储条件

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PERK inhibitor 28 (PERK-IN-5)

生物&药学活性

物理化学性质&存储条件

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