SD-208, also known as TGF-β RI Kinase Inhibitor V, is a novel protein kinase D inhibitor. SD-208 blocks prostate cancer cell proliferation and tumor growth in vivo by inducing G2/M cell cycle arrest. SD-208 reduces the development and progression of melanoma bone metastases. SD-208 inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo.
CAS Number: 627536-09-8
Molecular Weight: 352.75
TGF-β RI Kinase Inhibitor V
Chemical Name: 2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-4-pteridinamine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
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 blocks 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.
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).
- Fadakar P, Akbari A, Ghassemi F, Mobini GR, Mohebi M, Bolhassani M, Abed Khojasteh H, Heidari M. Evaluation of SD-208, a TGF-β-RI Kinase Inhibitor, as an Anticancer Agent in Retinoblastoma. Acta Med Iran. 2016 Jun;54(6):352-8. PubMed PMID: 27306340.
- Akbari A, Ghahremani MH, Mobini GR, Abastabar M, Akhtari J, Bolhassani M, Heidari M. Down-regulation of miR-135b in colon adenocarcinoma induced by a TGF-β receptor I kinase inhibitor (SD-208). Iran J Basic Med Sci. 2015 Sep;18(9):856-61. PubMed PMID: 26523217; PubMed Central PMCID: PMC4620183.
- Li M, Fang Y, Yao M, Yu WR, Ni T, Gu C, Yang PG, Mao ZG. [Effects of transforming growth factor β1 receptor inhibitor SD-208 on human hypertrophic scar]. Zhonghua Shao Shang Za Zhi. 2016 Jul 20;32(7):389-95. doi: 10.3760/cma.j.issn.1009-2587.2016.07.002. Chinese. PubMed PMID: 27464628.
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