| Identification | Back Directory | [Name]
CS 7017 | [CAS]
223132-38-5 | [Synonyms]
CS 7017
RS5444 dihydrochloride
CS-7017 dihydrochloride
Inolitazone (CS-7017) 2HCl
Efatutazone dihydrochloride
Inolitazone (dihydrochloride)
Inolitazone (CS-7017) dihydrochloride
EFATUTAZONE; CS-7017; RS5444; CS 7017; RS 5444
5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methylbenzimidazol-2-yl]methoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
5-[[4-[[6-(4-Amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-thiazolidinedione dihydrochloride | [Molecular Formula]
C27H28Cl2N4O4S | [MDL Number]
MFCD13194772 | [MOL File]
223132-38-5.mol | [Molecular Weight]
575.507 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 25 mg/mL (43.44 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) | [form ]
Powder | [color ]
Pale purple to purple |
| Hazard Information | Back Directory | [Uses]
Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition. | [in vivo]
Inolitazone dihydrochloride (Efatutazone dihydrochloride) plus Paclitaxel demonstrate additive antiproliferative activity in cell culture and minimal ATC tumor growth. When Inolitazone is administered in the diet to athymic nude mice prior to DRO tumor cell implantation, tumor growth is inhibited in a dose responsive fashion. At the highest dose, 0.025% Inolitazone inhibits growth on day 32 by 94.4% as compared to that of control. In this treatment group, five of 10 animals do not develop demonstrable tumors. In the 0.0025% treatment group, tumor growth is inhibited by 62.3% compared to that of control on day 32 while the 0.00025% dose demonstrated no growth inhibitory activity as compared to control. Tumors is nest allowed to establish in the mouse and began 0.025% Inolitazone treatment of mice 1 week after DRO or ARO tumor cell implantation. Inolitazone treated animals demonstrate tumor growth inhibition of 68.9% in DRO tumors and 48.3% in ARO tumors as compared to that of their respective controls on day 35[1]. | [IC 50]
PPARγ | [References]
[1] Copland JA, et al. Novel high-affinity PPARgamma agonist alone and in combination with paclitaxel inhibits human anaplastic thyroid carcinoma tumor growth via p21WAF1/CIP1. Oncogene. 2006 Apr 13;25(16):2304-17. DOI:10.1038/sj.onc.1209267
[2] Marlow LA, et al. Reactivation of suppressed RhoB is a critical step for the inhibition of anaplastic thyroid cancer growth. Cancer Res. 2009 Feb 15;69(4):1536-44. DOI:10.1158/0008-5472.CAN-08-3718 |
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| Company Name: |
LETOPHARM LIMITED
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| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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