[CAS NO. 627536-09-8]  SD-208

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PRODUCTS SPECIFICATIONS [627536-09-8]

Catalog
SLK-S7624
Brand
Selleck
CAS
627536-09-8

DESCRIPTION [627536-09-8]

Overview

MDLMFCD11519969
Molecular Weight352.75
Molecular FormulaC17H10ClFN6
SMILESFC1=CC=C(Cl)C=C1C2=NC(NC3=CC=NC=C3)=C4N=CC=NC4=N2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.8349 mL14.1743 mL28.3487 mL
5 mM0.5670 mL2.8349 mL5.6697 mL
10 mM0.2835 mL1.4174 mL2.8349 mL
50 mM---

Description

SD-208 is a selective inhibitor with of 48 nM, >100-fold selectivity over TGF-βRII.

Targets

TGF-βRI (ALK5) [1]
(Cell-free assay)
48 nM

In vitro

SD-208 inhibits the cell growth and constitutive and TGF-beta-evoked migration and invasion, and enhances immunogenicity in murine SMA-560 and human LN-308 glioma cells. SD-208 blocka TGF-beta-induced phosphorylation of the receptor-associated Smads, Smad2 and Smad3, and stimulates epithelial-to-mesenchymal transdifferentiation, migration, and invasiveness into Matrigel in vitro. SD-208 also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro.

In vivo

SD-208 (1 mg/mL, p.o.) significantly prolongs the median survival of SMA-560 glioma-bearing mice. In syngeneic 129S1 mice, SD-208 (60 mg/kg/d, p.o.) inhibits primary R3T tumor growth, and reduces the number and the size of lung metastases. In the murine aortic allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA).