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Bimiralisib (PQR309) - 98%, high purity , CAS No.1225037-39-7, Inhibitor of mechanistic target of rapamycin kinase;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;

COA COA
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Item Number
B414146
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B414146-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$107.90
B414146-10mg
10mg
3
$151.90
B414146-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$342.90
B414146-50mg
50mg
3
$478.90
B414146-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$804.90
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p110δ Selective Inhibitors

View related series
mechanistic target of rapamycin kinase Inhibitor (46) mTOR (145) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit alpha Inhibitor (76) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit beta Inhibitor (60) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit delta Inhibitor (71) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit gamma Inhibitor (69) PI3K (243) PI3K/Akt/mTOR (765)

Basic Description

Synonyms AS-49856 | GTPL8383 | UNII-6Z3QHB00LB | PQR309; Bimiralisib free base | s8738 | BCP15887 | PQR 309 | Q27088437 | 5-(4,6-Di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-2-pyridinamine | NSC785117 | NSC-785117 | A3W | Bimiralisib [USAN:INN:WHO-DD]
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of mechanistic target of rapamycin kinase;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;
Product Description

Information

Bimiralisib (PQR309) is a novel brain-penetrant dualPI3K/mTORinhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.


Targets

PI3Kα (Cell-free assay); PI3Kβ (Cell-free assay); mTOR (Cell-free assay); PI3Kγ (Cell-free assay); PI3Kδ (Cell-free assay) 1.5 nM(Kd); 11 nM(Kd); 12 nM(Kd); 25 nM(Kd); 25 nM(Kd)


In vitro

PQR309 shows in vitro activity with a median IC50 value of 233 nmol/L (95% CI, 174-324 nmol/L) in most of the tesed lymphoma cell lines (increasing doses, 72 hours). The arrest in proliferation is mainly due to cell cycle arrest with a block in G1 rather than to apoptosis, limited to only 2/7 cell lines. PQR309 is more active in B-cell lymphoma cell lines (DLBCL, MCL, CLL, and SMZL) than in the T-cell derived ALCL. PQR309 inhibits PI3K/mTOR signaling in lymphoma cell lines. It has in vitro and in vivo antilymphoma activity as single agent and in combination.\xa0


In vivo

PQR309 is orally available, crosses the blood−brain barrier, and displayed favorable pharmacokinetic parameters in mice, rats, and dogs. It shows little clearance when exposed to rat, dog, and human liver microsomes, with a quicker turnover of PQR309 in mouse liver microsomes, where 40% of the compound was eliminated within 30 min. In female mice, plasma concentrations of PQR309 depended on the drug administration route, resulting in half-lives of approximately 13-36 min for po administration vs 9-10 min for iv administration. PQR309 shows excellent oral bioavailability (>50%). Male Beagle dogs, exposed to PQR309 at 10 mg/kg po, showed maximal drug plasma concentrations Cmax of 583 ng/mL (approximately 1.5 μM) after 60-90 min and a half-life of >7 h, which results in drug levels of approximately 0.38 μM (150 ng/mL) after 24 h. The oral bioavailability in male Beagle dogs was estimated to be 23%. Altogether the PK studies in the three models (female CD-1 mouse, female Sprague-Dawley rats, male Beagle dog) show rapid absorption of PQR309 and good oral bioavailability. PQR309 demonstrates efficiency in inhibiting proliferation in tumor cell lines (PC3 prostate cancer cells) and a rat xenograft model (PC3 xenograft model).


Cell Research(from reference)

Cell lines：lymphoma cell lines 

Concentrations：500 nmol/L 

Incubation Time：72 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Triazines
Subclass Aminotriazines
Intermediate Tree Nodes Not available
Direct Parent 1,3,5-triazine-2,4-diamines
Alternative Parents Dialkylarylamines  Aminopyridines and derivatives  Morpholines  Imidolactams  1,3,5-triazines  Heteroaromatic compounds  Oxacyclic compounds  Dialkyl ethers  Azacyclic compounds  Primary amines  Organofluorides  Hydrocarbon derivatives  Alkyl fluorides  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents 2,4-diamine-s-triazine - Dialkylarylamine - Aminopyridine - Morpholine - Oxazinane - Pyridine - 1,3,5-triazine - Imidolactam - Heteroaromatic compound - Tertiary amine - Dialkyl ether - Ether - Oxacycle - Azacycle - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Organic oxygen compound - Alkyl halide - Alkyl fluoride - Hydrocarbon derivative - Primary amine - Amine - Organic nitrogen compound - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as 1,3,5-triazine-2,4-diamines. These are aromatic compounds containing a 1,3,5-triazine ring which is 2,4-disusbtituted wit amine groups.
External Descriptors Not available

Associated Targets(Human)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CD Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MTOR Tclin Serine/threonine-protein kinase mTOR (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKDC Tchem DNA-dependent protein kinase (1929 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CD Tclin PI3-kinase p110-delta subunit (6699 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PI4KB Tchem PI4-kinase beta subunit (1593 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CB Tchem PI3-kinase p110-beta subunit (4044 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A2058 (690 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OVCAR-3 (48710 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PC-3 (62116 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SK-OV-3 (52876 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3C2B Tchem Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide (438 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver (3974 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3C3 Tchem Phosphatidylinositol 3-kinase catalytic subunit type 3 (535 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3R1 Tchem PI3-kinase p110-alpha/p85-alpha (2589 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MTOR Tclin mTORC1 (330 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

PIK3CA PI3-kinase p110-alpha subunit (51 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Canis familiaris (36305 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Brain (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504771693
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504771693
IUPAC Name 5-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine
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)
InChIKey ADGGYDAFIHSYFI-UHFFFAOYSA-N
Smiles C1COCCN1C2=NC(=NC(=N2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4
Isomeric SMILES C1COCCN1C2=NC(=NC(=N2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4
Alternate CAS 1225037-39-7
Molecular Weight 411.38
Reaxy-Rn 20245212
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20245212&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

2 results found

Lot Number Certificate Type Date Item
H2205828 Certificate of Analysis May 12, 2025 B414146
H2205873 Certificate of Analysis May 12, 2025 B414146

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 6 mg/mL (14.58 mM); Water: Insoluble; Ethanol: Insoluble;
Molecular Weight 411.400 g/mol
XLogP3 1.300
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 12
Rotatable Bond Count 3
Exact Mass 411.163 Da
Monoisotopic Mass 411.163 Da
Topological Polar Surface Area 103.000 Ų
Heavy Atom Count 29
Formal Charge 0
Complexity 506.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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