SD 208

TGF-beta is a cell growth and differentiation factor that has roles in cancer, fibrosis, and numerous other pathologies. TGF-beta signals through two receptor tyrosine kinases, TGF-betaRI and TGF-betaRII. SD 208 is a potent inhibitor of TGF-betaRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of other tyrosine or serine/threonine kinases, including TGF-betaRII kinase. It blocks both autocrine and paracrine TGF-beta signaling in glioma cells, inhibiting TGF-beta-induced migration and invasion without affecting viability or proliferation. SD 208 is orally bioavailable and prevents TGF-beta-induced Smad phosphorylation in spleens and brains of mice. 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. SD 208 also suppresses TGF-beta-induced differentiation of proliferating myofibroblasts and induces dedifferentiation in the absence of TGF-beta.Formal Name: 2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-4-pteridinamine. CAS Number: 627536-09-8. Synonyms: TGF-beta RI Kinase Inhibitor V. Molecular Formula: C17H10ClFN6. Formula Weight: 352.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.3 mg/ml. lambdamax: 205, 258, 362 nm. SMILES: ClC1=CC=C(F)C(C2=NC(N=CC=N3)=C3C(NC4=CC=NC=C4)=N2)=C1. InChi Code: 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.