PQR-309 is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PQR-309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.
CAS Number: 1225037-39-7
Molecular Weight: 411.38
Bimiralisib free base
Related CAS Number:
Chemical Name: 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
PQR-309 is a highly selective pan-PI3K inhibitor with a balanced targeting of mTOR kinase. PQR-309 also inhibits PI3Kα-H1047R), PI3Kα-E542K and PI3Kα-E545K with IC50s of 36 nM, 63 nM and 136 nM, respectively.
Oral administration yields similar concentrations of PQR-309 in brain and plasma samples illustrates that PQR-309 readily passes the blood–brain barrier. In mice, both po and iv application routes show a rapid drop below 200 ng/mL (~0.5 μM) of PQR-309 within <1 h (iv) to <2 h (po) after administration, which reflects the time point when the drug reaches the median GI50 determined in tumor cell lines. In female rats a single oral dose (10 mg/kg) achieves similar drug levels as a single intravenous injection (5 mg/kg) with regard to Cmax. The half-life of 5-8 h and an AUC0.25-12 of around 14 000 h•ng/mL contributed to an excellent oral bioavailability of PQR-309 (>50%). Twenty-four hours after po administration, plasma levels of PQR-309 are still >2 μM (800-1000 ng/mL). Moreover, after 1-2 h exposure to PQR-309 , drug levels in rat brain samples are comparable to plasma levels, confirming rapid access of PQR-309 to the brain.
- Big Hopes with Small Molecules - PIQUR Therapeutics AG is aiming to Turn Cancer into a Manageable Disease. Chimia (Aarau). 2014 Dec;68(12):891-2. doi: 10.2533/chimia.2014.891. PubMed PMID: 26508614.
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