PQR-309


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

Description

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.

Product information

CAS Number: 1225037-39-7

Molecular Weight: 411.38

Formula: C17H20F3N7O2

Synonym:

Bimiralisib free base

PQR309

PQR-309

Related CAS Number:

1820902-72-4 (HCl)

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

Smiles: NC1=CC(=C(C=N1)C1N=C(N=C(N=1)N1CCOCC1)N1CCOCC1)C(F)(F)F

InChiKey: ADGGYDAFIHSYFI-UHFFFAOYSA-N

InChi: 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)

Technical Data

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

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.

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed