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SD208

SD208

  • CAT Number: I004365
  • CAS Number: 627536-09-8
  • Molecular Formula: C₁₇H₁₀ClFN₆
  • Molecular Weight: 352.75
  • Purity: ≥95%
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SD208 (CAT: I004365) is a selective inhibitor of transforming growth factor-beta (TGF-β) receptor I (ALK5) kinase. It has been reported to inhibit TGF-β signaling and attenuate the phosphorylation of SMAD2, a downstream effector of the TGF-β signaling pathway. SD208 has demonstrated potential in various preclinical studies for its anti-fibrotic, anti-inflammatory, and anti-tumor activities. It may have applications in the treatment of diseases associated with aberrant TGF-β signaling, such as fibrosis, cancer, and autoimmune disorders.

Catalog Number I004365
CAS Number 627536-09-8
Synonyms

2-(5-chloro-2-fluorophenyl)-N-pyridin-4-ylpteridin-4-amine

Molecular Formula

C₁₇H₁₀ClFN₆

Purity 95%
Target TGF-βR1(ALK5)
Solubility DMSO >10 mg/mL
Storage Store at -20°C
Related CAS 1608481-61-3 (hydrochloride)
IC50 49 nM
InChI 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)
InChIKey BERLXWPRSBJFHO-UHFFFAOYSA-N
SMILES C1=CC(=C(C=C1Cl)C2=NC3=NC=CN=C3C(=N2)NC4=CC=NC=C4)F
Reference

1:[Effects of transforming growth factor β1 receptor inhibitor SD-208 on human hypertrophic scar]. Li M, Fang Y, Yao M, Yu WR, Ni T, Gu C, Yang PG, Mao ZG.Zhonghua Shao Shang Za Zhi. 2016 Jul 20;32(7):389-95. doi: 10.3760/cma.j.issn.1009-2587.2016.07.002. Chinese. PMID: 27464628 <br />
2:Evaluation of SD-208, a TGF-β-RI Kinase Inhibitor, as an Anticancer Agent in Retinoblastoma. Fadakar P, Akbari A, Ghassemi F, Mobini GR, Mohebi M, Bolhassani M, Abed Khojasteh H, Heidari M.Acta Med Iran. 2016 Jun;54(6):352-8. PMID: 27306340 Free Article<br />
3:Down-regulation of miR-135b in colon adenocarcinoma induced by a TGF-β receptor I kinase inhibitor (SD-208). Akbari A, Ghahremani MH, Mobini GR, Abastabar M, Akhtari J, Bolhassani M, Heidari M.Iran J Basic Med Sci. 2015 Sep;18(9):856-61. PMID: 26523217 Free PMC Article<br />
4:SD-208, a novel protein kinase D inhibitor, blocks prostate cancer cell proliferation and tumor growth in vivo by inducing G2/M cell cycle arrest. Tandon M, Salamoun JM, Carder EJ, Farber E, Xu S, Deng F, Tang H, Wipf P, Wang QJ.PLoS One. 2015 Mar 6;10(3):e0119346. doi: 10.1371/journal.pone.0119346. eCollection 2015. PMID: 25747583 Free PMC Article<br />
5:Evaluation of antitumor activity of a TGF-beta receptor I inhibitor (SD-208) on human colon adenocarcinoma. Akbari A, Amanpour S, Muhammadnejad S, Ghahremani MH, Ghaffari SH, Dehpour AR, Mobini GR, Shidfar F, Abastabar M, Khoshzaban A, Faghihloo E, Karimi A, Heidari M.Daru. 2014 Jun 5;22:47. doi: 10.1186/2008-2231-22-47. PMID: 24902843 Free PMC Article<br />
6:Inhibition of intimal hyperplasia in murine aortic allografts by the oral administration of the transforming growth factor-beta receptor I kinase inhibitor SD-208. Sun Y, Ye P, Wu J, Liu Z, Zhang A, Ren L, Cheng C, Huang X, Wang K, Deng P, Wu C, Yue Z, Xia J.J Heart Lung Transplant. 2014 Jun;33(6):654-61. doi: 10.1016/j.healun.2014.02.020. Epub 2014 Feb 21. PMID: 24685405 <br />
7:TGF-beta-RI kinase inhibitor SD-208 reduces the development and progression of melanoma bone metastases. Mohammad KS, Javelaud D, Fournier PG, Niewolna M, McKenna CR, Peng XH, Duong V, Dunn LK, Mauviel A, Guise TA.Cancer Res. 2011 Jan 1;71(1):175-84. doi: 10.1158/0008-5472.CAN-10-2651. Epub 2010 Nov 16. Erratum in: Cancer Res. 2011 Mar 1;71(5):2023. PMID: 21084275 Free PMC Article<br />
8:Effect of transforming growth factor-beta receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling. Leung SY, Niimi A, Noble A, Oates T, Williams AS, Medicherla S, Protter AA, Chung KF.J Pharmacol Exp Ther. 2006 Nov;319(2):586-94. Epub 2006 Aug 3. PMID: 16888081 Free Article<br />
9:SD-208, a novel transforming growth factor beta receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Uhl M, Aulwurm S, Wischhusen J, Weiler M, Ma JY, Almirez R, Mangadu R, Liu YW, Platten M, Herrlinger U, Murphy A, Wong DH, Wick W, Higgins LS, Weller M.Cancer Res. 2004 Nov 1;64(21):7954-61. PMID: 15520202 Free Article

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