A potent inhibitor of TGF-βRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of other kinases; blocks both autocrine and paracrine TGF-β signaling in glioma cells; is orally bioavailable and prevents TGF-β-induced Smad phosphorylation in spleens and brains of mice

SD 208 – 10 mg

Brand:
Cayman
CAS:
627536-09-8
Storage:
-20
UN-No:
Non-Hazardous - /

TGF-β is a cell growth and differentiation factor that has roles in cancer, fibrosis, and numerous other pathologies.{20609,17350} TGF-β signals through two receptor tyrosine kinases, TGF-βRI and TGF-βRII. SD 208 is a potent inhibitor of TGF-βRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of other tyrosine or serine/threonine kinases, including TGF-βRII kinase.{27141} It blocks both autocrine and paracrine TGF-β signaling in glioma cells, inhibiting TGF-β-induced migration and invasion without affecting viability or proliferation.{27141} SD 208 is orally bioavailable and prevents TGF-β-induced Smad phosphorylation in spleens and brains of mice.{27141} It improves survival in mice with xenografted glioma by heightening the immune response against tumor cells and reverses bronchial hyperresponsiveness to allergens in ovalbumin-exposed mice.{27141,27142} SD 208 also suppresses TGF-β-induced differentiation of proliferating myofibroblasts and induces dedifferentiation in the absence of TGF-β.{27144,27143}  

 

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Description

A potent inhibitor of TGF-βRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of other kinases; blocks both autocrine and paracrine TGF-β signaling in glioma cells; is orally bioavailable and prevents TGF-β-induced Smad phosphorylation in spleens and brains of mice

Formal name: 2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-4-pteridinamine

Synonyms:  TGF-β RI Kinase Inhibitor V

Molecular weight: 352.8

CAS: 627536-09-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Activin-like Kinases (ALKs)||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling||Research Area|Cell Biology|Cell Signaling||Research Area|Immunology & Inflammation|Allergy||Research Area|Neuroscience

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