G5-7 - ≥99% , CAS No.939681-36-4

CAS: 939681-36-4 Cat. No.: G646574 Peso molecular: 411.4 PubChem CID: 73553353

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068 ) and STAT3 by binding to JAK2 . G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study

In Vitro

G5-7 (0-5 μM) inhibits EGFR tyrosine phosphorylation and downstream mTOR signaling and arrests the cell cycle at G2 phase. G5-7 does not directly inhibit EGFR activation. G5-7 (0-10 μM) comparably increases the abundance of markers (cleved-PARP and caspase 3) of apoptosis in parental LN229 cells and U87MG/EGFRvIII cells. G5-7 interacts with full-length JAK2. G5-7 significantly inhibits EGFR Tyr1068 phosphorylation but had no effect on EGFR Tyr1045 phosphorylation. G5-7 downregulates the downstream signaling of JAK by mTOR. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot Analysis. Cell Line: U87MG/PTEN cells. Concentration: 0-5 μM. Incubation Time: 6 hours. Result: Blocked EGFR phosphorylation and cell cycle at G2 phase to inhibit cell proliferation.

In Vivo

G5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Cells (4 × 10 6 ) in 100 μl of serum-free DMEM were inoculated subcutaneously into 5- to 6-week-old female nude mice . Dosage: 10 and 50 mg/kg. Administration: Oral gavage. Result: Suppresses angiogenesis in tumors.

Form:Solid

IC50& Target:JAK2

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068 ) and STAT3 by binding to JAK2 . G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

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Tipo de acción

INHIBITOR

Pureza

≥99%

Nombres e identificadores

• Sonrisas canónicas: CC(C)(C)OC(=O)N1CC(=CC2=CC=CC=C2F)C(=O)C(=CC3=CC=CC=C3F)C1
• IUPAC Name: tert-butyl (3Z,5Z)-3,5-bis[(2-fluorophenyl)methylidene]-4-oxopiperidine-1-carboxylate
• InChIKey: MCSPIRBNMDODQP-BKHHGCLFSA-N
• INCHI: 1S/C24H23F2NO3/c1-24(2,3)30-23(29)27-14-18(12-16-8-4-6-10-20(16)25)22(28)19(15-27)13-17-9-5-7-11-21(17)26/h4-13H,14-15H2,1-3H3/b18-12-,19-13-
• Isómeros SMILES: CC(OC(=O)N1C/C(=C/C2=CC=CC=C2F)/C(=O)/C(=C\C3=CC=CC=C3F)/C1)(C)C
• PubChem CID: 73553353
• Peso molecular: 411.4

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Organoheterocyclic compounds
    • Clase Piperidines
      • Subclass Piperidinecarboxylic acids and derivatives

• Kingdom: Organic compounds
• Superclass: Organoheterocyclic compounds
• Clase: Piperidines
• Subclass: Piperidinecarboxylic acids and derivatives
• Intermediate Tree Nodes: Not available
• Direct Parent: Piperidinecarboxylic acids
• Alternative Parents: Piperidinones Fluorobenzenes Aryl fluorides Carbamate esters Cyclic ketones Azacyclic compounds Organonitrogen compounds Organofluorides Organic oxides Hydrocarbon derivatives
• Molecular Framework: Aromatic heteromonocyclic compounds
• Substituents: Piperidinecarboxylic acid - Fluorobenzene - Halobenzene - Piperidinone - Aryl fluoride - Aryl halide - Monocyclic benzene moiety - Benzenoid - Carbamic acid ester - Ketone - Cyclic ketone - Azacycle - Hydrocarbon derivative - Organic oxide - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Organic oxygen compound - Organic nitrogen compound - Carbonyl group - Aromatic heteromonocyclic compound
• Descripción: This compound belongs to the class of organic compounds known as piperidinecarboxylic acids. These are compounds containing a piperidine ring which bears a carboxylic acid group.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Propiedades químicas y físicas

• Solubilidad: DMSO : 83.33 mg/mL (217.35 mM; Need ultrasonic)