AS2863619 free base - ≥99% , CAS No.2241300-50-3

CAS: 2241300-50-3 Cat. No.: A649143 Peso molecular: 332.32 PubChem CID: 139600292

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (T reg ) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC 50 s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19 , which consequently activates the Foxp3 gene

In Vitro

AS2863619 (1 μM; 22 hours; mouse CD4 + T cells) treatment suppresses serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Mouse CD4 + T cells Concentration: 1 μM Incubation Time: 22 hours Result: Suppressed serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples.

In Vivo

AS2863619 (30 mg/kg; oral administration; daily; for 2 weeks; mice) treatment after sensitization with 2,4-dinitrofluorobenzene (DNFB) dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of interferon-γ + (IFN-γ + ) cells in a skin contact hypersensitivity model, when compared with vehicle-treated control mice. T reg depletion before the elicitation of the secondary response abolishes AS2863619-induced suppression. KLRG1 + Foxp3 + T cells are specifically increased in DNFB sensitized AS2863619-treated mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice with DNFB-induced contact skin hypersensitivity Dosage: 30 mg/kg Administration: Oral administration; daily; for 2 weeks Result: The degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreased ratios of interferon-γ + (IFN-γ + ) cells.

Form:Solid

IC50& Target:CDK8 0.61 nM (IC 50 ) CDK19 4.28 nM (IC 50 ) GSK3α 76.67 nM (IC 50 ) GSK3β 63.06 nM (IC 50 ) STAT5

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (T reg ) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Pureza

≥99%

Nombres e identificadores

• Sonrisas canónicas: CC1=NC2=C(N1)C=C(C=C2)N3C4=C(C=NC=C4)N=C3C5=NON=C5N
• IUPAC Name: 4-[1-(2-methyl-3H-benzimidazol-5-yl)imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine
• InChIKey: OORKHRHPVSWORX-UHFFFAOYSA-N
• INCHI: 1S/C16H12N8O/c1-8-19-10-3-2-9(6-11(10)20-8)24-13-4-5-18-7-12(13)21-16(24)14-15(17)23-25-22-14/h2-7H,1H3,(H2,17,23)(H,19,20)
• PubChem CID: 139600292
• Peso molecular: 332.32

Propiedades químicas y físicas

• Solubilidad: DMSO : 250 mg/mL (752.29 mM; Need ultrasonic)
• Peso molecular: 332.320 g/mol
• XLogP3: 1.200
• Hydrogen Bond Donor Count: 2
• Hydrogen Bond Acceptor Count: 7
• Rotatable Bond Count: 2
• Exact Mass: 332.113 Da
• Monoisotopic Mass: 332.113 Da
• Topological Polar Surface Area: 124.000 Ų
• Heavy Atom Count: 25
• Formal Charge: 0
• Complexity: 495.000
• 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