PIK5-12d | PIKfyve PROTAC | Probechem Biochemicals

Chemical Structure : PIK5-12d

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PIK5-12d (PIKfyve PROTAC)

货号: PC-21468Not For Human Use, Lab Use Only.

PIK5-12d is a highly potent, selective, first-in-class PIKfyve PROTAC degrader, potently degrades PIKfyve protein with DC50 value of 1.48 nM and Dmax value of 97.7% in prostate cancer VCaP cells.

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1 mg	￥2280	In stock
5 mg	￥4780	In stock
10 mg		Get quote
25 mg		Get quote

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生物&药学活性

PIK5-12d is a highly potent, selective, first-in-class PIKfyve PROTAC degrader, potently degrades PIKfyve protein with DC50 value of 1.48 nM and Dmax value of 97.7% in prostate cancer VCaP cells.
PIK5-12d (100 nM) causes fast degradation of PIKfyve protein with a t1/2 value of 1.5 h in VCaP cells, also effectively reduces PIKfyve in other prostate cancer PC3, LNCaP, and 22RV1 cells.
PIK5-12d is a highly specific PIKfyve degrader with only 3 proteins significantly downregulated including PIKfyve, which accounts for the off-target rate at 2 out of 7573 detectable proteins.
PIK5-12d is selective for PIKfyve over other lipid kinases.
PIK5-12d mediated-PIKfyve degradation is VHL and proteasome-dependent.
PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagy in prostate cancer cells.
PIK5-12d inhibits VCaP cell proliferation with an IC50 of 522.3 nM, exerts prolonged suppression of PIKfyve downstream signaling.
PIK5-12d (10 mg/kg) almost completely depleted PIKfyve protein in LTL-331R human prostate cancer patient-derived xenograft (PDX) model, significantly suppressed tumor proliferation in vivo.

物理化学性质&存储条件

分子量	973.21
分子式	C52H64N10O7S
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	N1-((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-N6-(4-(2-((4-(2-((E)-3-methylbenzylidene)hydrazineyl)-6-morpholinopyrimidin-2-yl)oxy)ethyl)phenyl)adipamide

参考文献

1. Chungen Li, et al. J Med Chem. 2023 Sep 14;66(17):12432-12445.

PIK5-12d (PIKfyve PROTAC)

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物理化学性质&存储条件

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PIK5-12d (PIKfyve PROTAC)

生物&药学活性

物理化学性质&存储条件

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