S7071
SD-208
≥98% (HPLC), powder
Synonym(s):
2-(5-Chloro-2-fluorophenyl)pteridin-4-yl]pyridin-4-yl-amine
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About This Item
Empirical Formula (Hill Notation):
C17H10ClFN6
CAS Number:
Molecular Weight:
352.75
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
off-white to tan
solubility
DMSO: >5 mg/mL
storage temp.
2-8°C
SMILES string
Fc1ccc(Cl)cc1-c2nc(Nc3ccncc3)c4nccnc4n2
InChI
1S/C17H10ClFN6/c18-10-1-2-13(19)12(9-10)15-24-16-14(21-7-8-22-16)17(25-15)23-11-3-5-20-6-4-11/h1-9H,(H,20,22,23,24,25)
InChI key
BERLXWPRSBJFHO-UHFFFAOYSA-N
Application
SD-208 was used to inhibit the activity of ALK5 kinase in bovine retinal vascular cells.2
Biochem/physiol Actions
SD-208 is TGF-βR I kinase inhibitor with IC50 =49 nM based on direct enzymatic assay of TGFRI kinase (ALK5) activity with a specificity of >100-fold against TGFRII and at least 17-fold over members of a panel of related protein kinases including p38a, p38b, p38d, JNK1, EGFR, MAPKAPK2, MKK6, ERK2, PKC, PKA, PKD, CDC2, and CaMKII.
SD-208 is a novel transforming growth factor beta receptor I (TGF-βR I) kinase inhibitor. SD-208 inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo.
SD-208 is an inhibitor of TGF β receptor 1 kinase that is reportedly effective against human malignant gliomas. It increases the lytic activity and tumor infiltration by polyclonal natural killer cells, CD8 T cells and macrophages.1
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
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Rob J Van Geest et al.
Investigative ophthalmology & visual science, 51(4), 1857-1865 (2009-12-05)
Purpose. An early hallmark of preclinical diabetic retinopathy is thickening of the capillary basal lamina (BL). TGF-beta, a multipotent cytokine acting through its receptors ALK5 and -1, has been postulated to be involved in this phenomenon. In light of this
Overexpression of smad7 blocks primary tumor growth and lung metastasis development in osteosarcoma.
Audrey Lamora et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 20(19), 5097-5112 (2014-08-12)
Osteosarcoma is the main malignant primary bone tumor in children and adolescents for whom the prognosis remains poor, especially when metastasis is present at diagnosis. Because transforming growth factor-β (TGFβ) has been shown to promote metastasis in many solid tumors
Elisa Ventura et al.
Journal of immunology (Baltimore, Md. : 1950), 198(12), 4569-4574 (2017-05-10)
Glioblastoma is the most common and aggressive intrinsic brain tumor in adults. Self-renewing, highly tumorigenic glioma-initiating cells (GIC) have been linked to glioma invasive properties, immunomodulation, and increased angiogenesis, leading to resistance to therapy. TGF-β signaling has been associated with