SD-208


Catalog No. size PriceQuantity
M6904-2 2mg solid $77
M6904-10 10mg solid $328

Description

Cas:627536-09-8

Product Information

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.

 

Chemical Formula: C17H10ClFN6

 

Exact Mass: 352.064

 

Molecular Weight: 352.7574

 

Elemental Analysis: C, 57.88; H, 2.86; Cl, 10.05; F, 5.39; N, 23.82

 

Synonym: 

 

TGF-β RI Kinase Inhibitor V

 

Chemical Name:

2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-4-pteridinamine

 

InChi Key:

BERLXWPRSBJFHO-UHFFFAOYSA-N

 

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)

 

Smiles Code:

FC1=CC=C(Cl)C=C1C2=NC(NC3=CC=NC=C3)=C4N=CC=NC4=N2

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

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[2]. SD-208 also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro.

 

In Vivo:

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).

 

 

References

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

  1. Tandon M, Salamoun JM, Carder EJ, Farber E, Xu S, Deng F, Tang H, Wipf P, Wang QJ. 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. PLoS One. 2015 Mar 6;10(3):e0119346. doi: 10.1371/journal.pone.0119346. eCollection 2015. PubMed PMID: 25747583; PubMed Central PMCID: PMC4352033.

 

  1. 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. Evaluation of antitumor activity of a TGF-beta receptor I inhibitor (SD-208) on human colon adenocarcinoma. Daru. 2014 Jun 5;22:47. doi: 10.1186/2008-2231-22-47. PubMed PMID: 24902843; PubMed Central PMCID: PMC4077684.

 

Products are for research use only. Not for human use.

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