SML1906
AS1517499
≥98% (HPLC), STAT6 inhibitor, powder
Synonym(s):
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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About This Item
Empirical Formula (Hill Notation):
C20H20ClN5O2
CAS Number:
Molecular Weight:
397.86
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
Product Name
AS1517499, ≥98% (HPLC)
Quality Level
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 moderately inhibits the expression of RhoA (ras homolog family member A). Overexpression of RhoA protein is associated with allergic bronchial asthma.
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Shinya Nagashima et al.
Bioorganic & medicinal chemistry, 15(2), 1044-1055 (2006-10-31)
The STAT6 (signal transducers and activators of transcription 6) protein is activated by interleukin (IL)-4 and IL-13, and plays an important role in T-helper cell 2 (Th2) differentiation. STAT6 might therefore be an excellent therapeutic target for various allergic conditions
Daniela F Quail et al.
Science (New York, N.Y.), 352(6288), aad3018-aad3018 (2016-05-21)
Macrophages accumulate with glioblastoma multiforme (GBM) progression and can be targeted via inhibition of colony-stimulating factor-1 receptor (CSF-1R) to regress high-grade tumors in animal models of this cancer. However, whether and how resistance emerges in response to sustained CSF-1R blockade
The proximal STAT6 and NF-κB sites are responsible for IL-13-and TNF-α-induced RhoA transcriptions in human bronchial smooth muscle cells.
Goto K, et al.
Pharmacological Research, 61(5), 466-472 (2010)
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML1906-25MG | 04061832639307 |
| SML1906-5MG | 04061832639314 |