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JTE-952 - 99%, high purity , CAS No.1255303-54-8

    Grade & Purity:
  • ≥99%
In stock
Item Number
J647907
Grouped product items
SKU Size
Availability
Price Qty
J647907-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$495.90
J647907-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$790.90

Basic Description

Specifications & Purity ≥99%
Biochemical and Physiological Mechanisms JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor ( CSF-1R or cFMS , type III receptor tyrosine kinase), with IC 50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mo
Storage Temp Store at 2-8°C,Protected from light,Desiccated
Shipped In
Wet ice
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor ( CSF-1R or cFMS , type III receptor tyrosine kinase), with IC 50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis

In Vivo

JTE-952 (3 mg/kg, p.o. once-daily) treatment reduces the overall progression of the clinical score, including inflammation and bone erosion in mouse model of collagen-induced arthritis (CIA model) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mouse model of collagen-induced arthritis (CIA model) . Dosage: 3 mg/kg. Administration: Oral once-daily. Result: Reduced the overall progression of the clinical score, including inflammation and bone erosion.

Form:Solid

IC50& Target:IC50: 13 nM (CSF1R), 261 nM (TrkA)

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Azetidines
Subclass Phenylazetidines
Intermediate Tree Nodes Not available
Direct Parent Phenylazetidines
Alternative Parents Pyridinecarboxylic acids and derivatives  Phenoxy compounds  2-heteroaryl carboxamides  Methoxybenzenes  Anisoles  Alkyl aryl ethers  Glycerol ethers  Tertiary carboxylic acid amides  Heteroaromatic compounds  Tertiary amines  Secondary alcohols  1,2-diols  Amino acids and derivatives  Dialkyl ethers  Azacyclic compounds  Hydrocarbon derivatives  Organic oxides  Primary alcohols  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents 3-phenylazetidine - Pyridine carboxylic acid or derivatives - Anisole - Phenol ether - 2-heteroaryl carboxamide - Methoxybenzene - Phenoxy compound - Alkyl aryl ether - Glycerol ether - Glycerolipid - Monocyclic benzene moiety - Pyridine - Benzenoid - Heteroaromatic compound - Tertiary carboxylic acid amide - Tertiary amine - Secondary alcohol - 1,2-diol - Carboxamide group - Amino acid or derivatives - Ether - Azacycle - Dialkyl ether - Carboxylic acid derivative - Amine - Organonitrogen compound - Organooxygen compound - Alcohol - Primary alcohol - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as phenylazetidines. These are polycyclic aromatic compounds containing a phenyl ring substituted with an azetidine ring.
External Descriptors Not available

Associated Targets(Human)

CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KIT Tclin Stem cell growth factor receptor (10667 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK2A1 Tchem Casein kinase II alpha (3512 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCZ Tchem Protein kinase C zeta (2414 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDPK1 Tchem 3-phosphoinositide dependent protein kinase-1 (3758 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IKBKB Tchem Inhibitor of nuclear factor kappa B kinase beta subunit (5554 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCG Tchem Protein kinase C gamma (2471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RAF1 Tclin Serine/threonine-protein kinase RAF (4169 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FLT1 Tclin Vascular endothelial growth factor receptor 1 (6262 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK2 Tclin Rho-associated protein kinase 2 (6206 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK9 Tchem c-Jun N-terminal kinase 2 (4655 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK10 Tchem c-Jun N-terminal kinase 3 (3396 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (4127 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MET Tclin Hepatocyte growth factor receptor (10718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCA Tchem Protein kinase C alpha (5923 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FYN Tclin Tyrosine-protein kinase FYN (5308 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LYN Tclin Tyrosine-protein kinase Lyn (4251 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK1 Tclin Nerve growth factor receptor Trk-A (7922 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKACA Tchem cAMP-dependent protein kinase alpha-catalytic subunit (3475 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ZAP70 Tchem Tyrosine-protein kinase ZAP-70 (2189 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK8 Tchem c-Jun N-terminal kinase 1 (5038 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDGFRA Tclin Platelet-derived growth factor receptor alpha (5682 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT1 Tchem Serine/threonine-protein kinase AKT (9192 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FLT3 Tclin Tyrosine-protein kinase receptor FLT3 (13481 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SGK1 Tchem Serine/threonine-protein kinase Sgk1 (2343 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSF1R Tclin Macrophage colony stimulating factor receptor (5179 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TEK Tclin Tyrosine-protein kinase TIE-2 (3348 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHEK1 Tchem Serine/threonine-protein kinase Chk1 (6846 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK12 Tchem MAP kinase p38 gamma (2776 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KARS1 Tchem Lysyl-tRNA synthetase (184 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK1 Tchem Cyclin-dependent kinase 1/cyclin B1 (1887 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem CDK2/Cyclin A2 (2260 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Prkcb Protein kinase C beta (2 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 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
Csf1r Macrophage colony-stimulating factor 1 receptor (491 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 [3-[4-[(4-cyclopropylphenyl)methoxy]-3-methoxyphenyl]azetidin-1-yl]-[4-[[(2S)-2,3-dihydroxypropoxy]methyl]pyridin-2-yl]methanone
INCHI InChI=1S/C30H34N2O6/c1-36-29-13-24(8-9-28(29)38-18-20-2-4-22(5-3-20)23-6-7-23)25-14-32(15-25)30(35)27-12-21(10-11-31-27)17-37-19-26(34)16-33/h2-5,8-13,23,25-26,33-34H,6-7,14-19H2,1H3/t26-/m0/s1
InChIKey LTTJGQBDGMNWHJ-SANMLTNESA-N
Smiles COC1=C(C=CC(=C1)C2CN(C2)C(=O)C3=NC=CC(=C3)COCC(CO)O)OCC4=CC=C(C=C4)C5CC5
Isomeric SMILES COC1=C(C=CC(=C1)C2CN(C2)C(=O)C3=NC=CC(=C3)COC[C@H](CO)O)OCC4=CC=C(C=C4)C5CC5
PubChem CID 49806372
MeSH Entry Terms (2S)-3-((2-((3-(4-(4-cyclopropylbenzyloxy)-3-methoxyphenyl)azetidine-1-yl)carbonyl)pyridin-4-yl)methoxy)propane-1,2-diol;JTE-952
Molecular Weight 518.60

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

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

Chemical and Physical Properties

Molecular Weight 518.600 g/mol
XLogP3 2.900
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 12
Exact Mass 518.242 Da
Monoisotopic Mass 518.242 Da
Topological Polar Surface Area 101.000 Ų
Heavy Atom Count 38
Formal Charge 0
Complexity 736.000
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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