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AMG319 - 10mM in DMSO, high purity , CAS No.1608125-21-8, 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;5-bisphosphate 3-kinase catalytic subunit delta;Inhi

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Item Number
A421930
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A421930-1ml
1ml
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$331.90

p110δ Selective Inhibitors

View related series
Compound libraries (12325)

Basic Description

Synonyms AMG319 | AMG-319 | 1608125-21-8 | (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine | 19DG7G1U5Q | J3.391.906I | AMG 319 | N-((1S)-1-(7-Fluoro-2-(2-pyridyl)quinoline-3-yl)ethyl)-9H-purine-6-amine | N-[(1S)-1-(7-fluoro-2-pyridin-2-ylquinolin-3-yl)et
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
Storage Temp Store at -80°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 phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit delta;Inhi
Product Description

Information

AMG319 is a potent and selectivePI3Kδinhibitor withIC50of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.

Targets

PI3Kδ ; PI3Kγ 18 nM; 850 nM

In vitro

AMG319 inhibits anti-IgM/CD40L-induced B cell proliferation with IC50 of 8.6 nM and reduces pAkt level with IC50 of 1.5 nM. AMG319 also inhibits anti-IgD-induce CD-69 expression in HWB.

In vivo

In female Lewis rats, AMG319 (3 mg/kg, p.o.) inhibits the KLH-induced inflammatory response by 88%. In the transgenic (IgMm) mice, AMG319 (, p.o.) inhibits in vivo pAKT with IC50 of 1.9 nM.

Cell Research(from reference)

Cell lines:PBMCs 

Incubation Time:72 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Pyridines and derivatives
Subclass Bipyridines and oligopyridines
Intermediate Tree Nodes Not available
Direct Parent Bipyridines and oligopyridines
Alternative Parents Haloquinolines  6-alkylaminopurines  Aminopyrimidines and derivatives  Imidolactams  Benzenoids  Aryl fluorides  Imidazoles  Heteroaromatic compounds  Azacyclic compounds  Organofluorides  Hydrocarbon derivatives  Amines  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Bipyridine - Haloquinoline - 6-alkylaminopurine - 6-aminopurine - Quinoline - Purine - Imidazopyrimidine - Aminopyrimidine - Aryl fluoride - Aryl halide - Imidolactam - Benzenoid - Pyrimidine - Heteroaromatic compound - Azole - Imidazole - Azacycle - Organonitrogen compound - Amine - Organic nitrogen compound - Hydrocarbon derivative - Organofluoride - Organohalogen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as bipyridines and oligopyridines. These are organic compounds containing two pyridine rings linked to each other.
External Descriptors Not available

Product Properties

ALogP 3.691
HBD Count 2
Rotatable Bond 4

Associated Targets(Human)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (1 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 (1 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 (1 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 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CD Tclin PI3-kinase p110-delta subunit (6699 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NR1I2 Tchem Pregnane X receptor (6667 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
PIK3CB Tchem PI3-kinase p110-beta subunit (4044 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 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
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Pik3cd Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (89 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

IUPAC Name N-[(1S)-1-(7-fluoro-2-pyridin-2-ylquinolin-3-yl)ethyl]-7H-purin-6-amine
INCHI InChI=1S/C21H16FN7/c1-12(28-21-19-20(25-10-24-19)26-11-27-21)15-8-13-5-6-14(22)9-17(13)29-18(15)16-4-2-3-7-23-16/h2-12H,1H3,(H2,24,25,26,27,28)/t12-/m0/s1
InChIKey KWRYMZHCQIOOEB-LBPRGKRZSA-N
Smiles CC(C1=C(N=C2C=C(C=CC2=C1)F)C3=CC=CC=N3)NC4=NC=NC5=C4NC=N5
Isomeric SMILES C[C@@H](C1=C(N=C2C=C(C=CC2=C1)F)C3=CC=CC=N3)NC4=NC=NC5=C4NC=N5
PubChem CID 68947304
Molecular Weight 385.4

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

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

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility 77
DMSO(mM) Max Solubility 199.7924235
Water(mg / mL) Max Solubility <1
Molecular Weight 385.400 g/mol
XLogP3 3.300
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 4
Exact Mass 385.145 Da
Monoisotopic Mass 385.145 Da
Topological Polar Surface Area 92.300 Ų
Heavy Atom Count 29
Formal Charge 0
Complexity 551.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
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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