627536-09-8

SD 208/SD-208

627536-09-8

编号ABP000300 化学名称SD 208/SD-208 英文名称 SD 208/SD-208 MDL: MFCD11519969 分子式C17H10ClFN6 分子量352.759 纯度 >98 %

化学名称 : SD 208/SD-208

CAS : 627536-09-8

英文名称: SD 208/SD-208

英文同义词: SD-208

同义词: SD-208

Solubility:Soluble to 20 mM in DMSO

Storage:Store at RT

Biologieal

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. tent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50 = 49nM). Displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively. Exhibits anti-inflammatory and antitumor activity.

Reference

Uhl et al (2004) SD-208, a novel transforming growth factor β feceptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogeneicity of murine and human glioma cells in vitro and in vivo. Cancer Res. 64 7954. Kapoun et al (2006) Transforming growth factor-β receptor type I receptor (TGFβRI) kinase activity but not p38 activation is required for TGFβRI-induced myofibroblast differentiation and profibrotic gene expression. Mol.Pharmacol. 70 518. Leung et al (2006) Effect of transforming growth factor-β receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling. J.Pharmacol.Exp.Ther. 319 586.

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