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Merck

SML1906

AS1517499

≥98% (HPLC), STAT6 inhibitor, powder

Sinónimos:

2-[[2-(3-Chloro-4-hydroxyphenyl)ethyl]amino]-4-[(phenylmethyl)amino]-5-pyrimidinecarboxamide, 4-(Benzylamino)-2-{[2-(3-chloro-4-hydroxyphenyl)ethyl]amino}pyrimidine-5-carboxamide

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Fórmula empírica (notación de Hill):
C20H20ClN5O2
Número CAS:
Peso molecular:
397.86
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Servicio técnico
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Nombre del producto

AS1517499, ≥98% (HPLC)

Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

SMILES string

ClC1=CC(CCNC2=NC=C(C(N)=O)C(NCC3=CC=CC=C3)=N2)=CC=C1O

InChI

1S/C20H20ClN5O2/c21-16-10-13(6-7-17(16)27)8-9-23-20-25-12-15(18(22)28)19(26-20)24-11-14-4-2-1-3-5-14/h1-7,10,12,27H,8-9,11H2,(H2,22,28)(H2,23,24,25,26)

InChI key

OZRMEKAUZBKTTC-UHFFFAOYSA-N

Biochem/physiol Actions

AS1517499 is a potent STAT6 (signal transducer and activator of transcription 6) inhibitor (IC50 = 21 nM against IL-4-dependent reporter activity) that selectively prevents anti-CD3- & IL-4-induced T-helper cell 2 (Th2) differentiation of mouse spleen T cells (IC50 = 2.3 nM), without affecting anti-CD3- & IL-12-induced Th1 differentiation. AS1517499 in vivo effecicacy is demonstrated in various animal models of immunological disorders, including the autoimmune Graves′ disease, antigen-induced bronchial hypercontractility (10 mg/kg i.p.). AS1517499 treatment (10 mg/kg/day i.p.) following early gliomagenesis blockage by a CSF-1R inhibitor is also shown to greatly prolong the survival rate when compared with CSF-1R inhibition alone in a murine model of PDGF-driven glioma (PDG).
AS1517499 is a potent STAT6 (signal transducer and activator of transcription 6) inhibitor.
AS1517499 moderately inhibits the expression of RhoA (ras homolog family member A). Overexpression of RhoA protein is associated with allergic bronchial asthma.


Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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