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PQR530

Cat. No. M9753

All AbMole products are for research use only, cannot be used for human consumption.

PQR530 Structure
Synonym:

PQR-530

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Quality Control & Documentation
Biological Activity

PQR530 is a highly potent dual pan-PI3K/mTORC1/2 inhibitor. PQR530 inhibited protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 µM. PQR530 showed excellent selectivity over a wide panel of kinases, as well as excellent selectivity versus unrelated receptor enzymes and ion channels. Moreover, PQR530 displayed potency in a panel of 44 cancer cell lines (NTRC OncolinesTM) to prevent cancer cell growth (mean value for GI50 of 426 nM). Oral application of PQR530 to mice resulted in a dose-proportional PK and demonstrated good oral bioavailability and excellent brain penetration.

Chemical Information
Molecular Weight 407.42
Formula C18H23F2N7O2
CAS Number 1927857-61-1
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Wiebke Theilmann, et al. Neuropharmacology. Novel brain permeant mTORC1/2 inhibitors are as efficacious as rapamycin or everolimus in mouse models of acquired partial epilepsy and tuberous sclerosis complex

[2] Birthe Gericke, et al. Neuropharmacology. Selective inhibition of mTORC1/2 or PI3K/mTORC1/2 signaling does not prevent or modify epilepsy in the intrahippocampal kainate mouse model

[3] Elisabeth Singer, et al. Neuropharmacology. Brain-penetrant PQR620 mTOR and PQR530 PI3K/mTOR inhibitor reduce huntingtin levels in cell models of HD

[4] Claudia Brandt, et al. Neuropharmacology. The novel, catalytic mTORC1/2 inhibitor PQR620 and the PI3K/mTORC1/2 inhibitor PQR530 effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy

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  Catalog
Abmole Inhibitor Catalog




Keywords: PQR530, PQR-530 supplier, PI3K, inhibitors, activators

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