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Merck
CN

S7071

SD-208

≥98% (HPLC), powder

别名:

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

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关于此项目

经验公式(希尔记法):
C17H10ClFN6
化学文摘社编号:
分子量:
352.75
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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InChI key

BERLXWPRSBJFHO-UHFFFAOYSA-N

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)

assay

≥98% (HPLC)

form

powder

color

off-white to tan

solubility

DMSO: >5 mg/mL

storage temp.

2-8°C

Quality Level

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

pictograms

Exclamation mark

hcodes

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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
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
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
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
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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