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
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
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
Related Categories
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
Signal Word
Warning
Hazard Statements
Precautionary Statements
Hazard Classifications
Acute Tox. 4 Oral
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Personal Protective Equipment
dust mask type N95 (US), Eyeshields, Gloves
Regulatory Information
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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
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
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
Martin Uhl et al.
Cancer research, 64(21), 7954-7961 (2004-11-03)
The cytokine transforming growth factor (TGF)-beta, by virtue of its immunosuppressive and promigratory properties, has become a major target for the experimental treatment of human malignant gliomas. Here we characterize the effects of a novel TGF-beta receptor (TGF-betaR) I kinase
Tanja Stüber et al.
Journal for immunotherapy of cancer, 8(1) (2020-04-19)
Immunotherapy with chimeric antigen receptor (CAR)-engineered T-cells is effective in some hematologic tumors. In solid tumors, however, sustained antitumor responses after CAR T-cell therapy remain to be demonstrated both in the pre-clinical and clinical setting. A perceived barrier to the
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