PQR-309


Catalog No. size PriceQuantity
M6611-2 2mg solid $113
M6611-10 10mg solid $431

Description

Cas:1225037-39-7 (free base)

Product Information

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.

 

Chemical Formula: C17H20F3N7O2

 

Exact Mass: 411.1631

 

Molecular Weight: 411.3892 

 

Elemental Analysis: C, 49.63; H, 4.90; F, 13.85; N, 23.83; O, 7.78

 

Synonym: 

 

PQR309

PQR-309

PQR309

Bimiralisib free base

 

Chemical Name:

5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine

 

InChi Key:

ADGGYDAFIHSYFI-UHFFFAOYSA-N

 

InChi Code:    InChI=1S/C17H20F3N7O2/c18-17(19,20)12-9-13(21)22-10-11(12)14-23-15(26-1-5-28-6-2-26)25-16(24-14)27-3-7-29-8-4-27/h9-10H,1-8H2,(H2,21,22)

 

Smiles Code:

NC1=NC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C(C(F)(F)F)=C1

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro

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.

 

In Vivo

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.

 

 

References

 

  1. 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.

 

Products are for research use only. Not for human use.

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