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MedKoo Cat#: 406817 | Name: SD-208
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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 Structure

SD-208
SD-208
CAS#627536-09-8

Theoretical Analysis

MedKoo Cat#: 406817

Name: SD-208

CAS#: 627536-09-8

Chemical Formula: C17H10ClFN6

Exact Mass: 352.0640

Molecular Weight: 352.76

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

Price and Availability

Size Price Availability Quantity
10mg USD 110.00 Ready to ship
25mg USD 220.00 Ready to ship
50mg USD 385.00 Ready to ship
100mg USD 650.00 Ready to ship
200mg USD 1,050.00 Ready to ship
500mg USD 2,250.00 Ready to ship
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Related CAS #
627536-09-8
Synonym
SD-208; SD 208; SD208; TGF-β RI Kinase Inhibitor V.
IUPAC/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
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
More Info
Biological target:
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
In vitro activity:
The results of this study suggest that SD-208 could be an alternative agent in retinoblastoma treatment. The anti-cancer effect of SD-208 may be exerted due to the regulation of specific miRNAs, at least in the retinoblastoma Y-79 cell line. Expression changes were observed in miRNAs 18a, 20a, 22 and 34a in response to SD-208 treatment, and SD-208 treated Y-79 cells had remarkable cell proliferation inhibition as compared to untreated cells. Reference: Acta Med Iran. 2016 Jun;54(6):352-8. https://pubmed.ncbi.nlm.nih.gov/27306340/
In vivo activity:
TGF-beta receptor I kinase inhibitors, such as SD-208, hold promise as novel therapeutic agents for treating human malignant gliomas. In syngeneic VM/Dk mice with intracranial SMA-560 gliomas, oral administration of SD-208 extended median survival. Although there were no significant changes in blood vessel formation, proliferation, or apoptosis were observed, SD-208 responders exhibited increased tumor infiltration by natural killer cells, CD8 T cells, and macrophages. Reference: Cancer Res. 2004 Nov 1;64(21):7954-61. https://pubmed.ncbi.nlm.nih.gov/15520202/
Solvent mg/mL mM
Solubility
DMSO 9.1 25.77
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 352.76 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
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. PMID: 27306340. 2. 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. PMID: 26523217; PMCID: PMC4620183. 3. 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. 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. Cancer Res. 2004 Nov 1;64(21):7954-61. doi: 10.1158/0008-5472.CAN-04-1013. PMID: 15520202. 4. Ge R, Rajeev V, Ray P, Lattime E, Rittling S, Medicherla S, Protter A, Murphy A, Chakravarty J, Dugar S, Schreiner G, Barnard N, Reiss M. Inhibition of growth and metastasis of mouse mammary carcinoma by selective inhibitor of transforming growth factor-beta type I receptor kinase in vivo. Clin Cancer Res. 2006 Jul 15;12(14 Pt 1):4315-30. doi: 10.1158/1078-0432.CCR-06-0162. PMID: 16857807.
In vitro protocol:
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. PMID: 27306340. 2. 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. PMID: 26523217; PMCID: PMC4620183.
In vivo protocol:
1. 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. 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. Cancer Res. 2004 Nov 1;64(21):7954-61. doi: 10.1158/0008-5472.CAN-04-1013. PMID: 15520202. 2. Ge R, Rajeev V, Ray P, Lattime E, Rittling S, Medicherla S, Protter A, Murphy A, Chakravarty J, Dugar S, Schreiner G, Barnard N, Reiss M. Inhibition of growth and metastasis of mouse mammary carcinoma by selective inhibitor of transforming growth factor-beta type I receptor kinase in vivo. Clin Cancer Res. 2006 Jul 15;12(14 Pt 1):4315-30. doi: 10.1158/1078-0432.CCR-06-0162. PMID: 16857807.
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. 2: 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. 3: 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. 4: 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. 5: 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. 6: 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. Inhibition of intimal hyperplasia in murine aortic allografts by the oral administration of the transforming growth factor-beta receptor I kinase inhibitor SD-208. J Heart Lung Transplant. 2014 Jun;33(6):654-61. doi: 10.1016/j.healun.2014.02.020. Epub 2014 Feb 21. PubMed PMID: 24685405. 7: Mohammad KS, Javelaud D, Fournier PG, Niewolna M, McKenna CR, Peng XH, Duong V, Dunn LK, Mauviel A, Guise TA. TGF-beta-RI kinase inhibitor SD-208 reduces the development and progression of melanoma bone metastases. 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. PubMed PMID: 21084275; PubMed Central PMCID: PMC3225124. 8: Leung SY, Niimi A, Noble A, Oates T, Williams AS, Medicherla S, Protter AA, Chung KF. Effect of transforming growth factor-beta receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling. J Pharmacol Exp Ther. 2006 Nov;319(2):586-94. Epub 2006 Aug 3. PubMed PMID: 16888081. 9: 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. 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. Cancer Res. 2004 Nov 1;64(21):7954-61. PubMed PMID: 15520202.