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Key Documents

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S7071

Sigma-Aldrich

SD-208

≥98% (HPLC), powder

Sinónimos:

2-(5-Chloro-2-fluorophenyl)pteridin-4-yl]pyridin-4-yl-amine

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About This Item

Fórmula empírica (notación de Hill):
C17H10ClFN6
Número de CAS:
627536-09-8
Peso molecular:
352.75
MDL number:
MFCD11519969
UNSPSC Code:
12352200
PubChem Substance ID:
24899731
NACRES:
NA.77

Quality Level

100

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 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

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Katharina Seystahl et al.
Neuro-oncology, 17(2), 254-265 (2014-08-29)
The transforming growth factor (TGF)-β and vascular endothelial growth factor (VEGF) pathways have a major role in the pathogenesis of glioblastoma, notably immunosuppression, migration, and angiogenesis, but their interactions have remained poorly understood. We characterized TGF-β pathway activity in 9
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
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
Chandan K Nagaraju et al.
Scientific reports, 9(1), 8879-8879 (2019-06-22)
After myocardial infarction, resident fibroblasts (Fb) differentiate towards myofibroblasts (MyoFb), generating the scar tissue and the interstitial fibrosis seen in the adjacent myocardium. Fb and MyoFb have the potential to interact with cardiac myocytes (CMs) but insight into the phenotype-specific
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
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