AMG319 - 10mM in DMSO, high purity , CAS No.1608125-21-8

Item Number
A421930
Grouped product items
SKUSizeAvailabilityPrice Qty
A421930-1ml
1ml
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$331.90

p110δ Selective Inhibitors

Basic Description

SynonymsAMG319 | 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 & PurityMoligand™, 10mM in DMSO
Biochemical and Physiological MechanismsAMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
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 

Product Properties

ALogP3.691
HBD Count2
Rotatable Bond4

Associated Targets(Human)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIK3CD Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIK3CD Tclin PI3-kinase p110-delta subunit (6699 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NR1I2 Tchem Pregnane X receptor (6667 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIK3CB Tchem PI3-kinase p110-beta subunit (4044 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
B cell (126 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

PIK3CA PI3-kinase p110-alpha subunit (51 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Pik3cd Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (89 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

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
InChi Key KWRYMZHCQIOOEB-LBPRGKRZSA-N
Canonical 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

Certificate of Analysis(COA)

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Chemical and Physical Properties

DMSO(mg / mL) Max Solubility77
DMSO(mM) Max Solubility199.7924235
Water(mg / mL) Max Solubility<1

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