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| Product | Description | |
|---|---|---|
| Inolitazone | Inolitazone is an orally bioavailable PAPR-gamma inhibitor with potential antineoplastic activity. Inolitazone binds to and activates peroxisome proliferation-activated receptor gamma (PPAR-gamma), which may result in the induction of tumor cell differentiation and apoptosis, and so a reduction in tumor cell proliferation. PPAR-gamma is a nuclear hormone receptor and ligand-activated transcription factor controlling gene expression involved in such cellular processes as differentiation, apoptosis, cell-cycle control, carcinogenesis, and inflammation. Synonyms: CS-7017, CS7017; CS 7017; RS5444; RS-5444; RS 5444; Efatutazone; PPAR-gamma agonist CS-7017, CS-7017, RS5444. Efatutazone. CAS No. 223132-37-4. Molecular formula: C27H26N4O4S. Mole weight: 502.58. |  |
| Inolitazone dihydrochloride | In vitro, the IC50 for growth inhibition is approximately 0.8 nM while anaplastic thyroid carcinoma (ATC) tumor growth was inhibited three- to fourfold in nude mice. siRNA against PPARgamma and a pharmacological antagonist demonstrated that functional PPARgamma was required for growth inhibitory activity of RS5444. RS5444 upregulated the cell cycle kinase inhibitor, p21WAF1/CIP1. RS5444inhibited culture growth and caused irreversible G1 arrest, but did not induce apoptosis. In addition, RS5444 caused dramatic changes in cellular morphology which were associated with increased motility and diminished cellular adherence, but no increase in the ability of such cells to digest and invade Matrigel. Treatment with RS5444 leads to the up-regulation of RhoB and subsequent activation of p21, and that silencing of RhoB by RNAi blocks the ability of RS5444 to induce p21 and to inhibit ATC cells proliferation. The median peak efatutazone blood level was 8.6 ng/mL for 0.15-mg dosing vs 22.0 ng/mL for 0.3-mg twice daily dosing. Although efatutazone treatment did not reduce percentage of mice developing invasive cancer, it significantly reduced prevalence of noninvasive cancer and total number of cancers per mouse and increased prevalence of well-differentiated cancer subtypes not usually seen in this mouse model. Uses: Antineoplastic agents. Synonyms: Efatutazone; Efatutazone hydrochloride; CS 7017; CS-7017; CS7017 ;RS-5444; RS5444; UNII-76B44WEA8O. Grades: >98%. CAS No. 223132-38-5. Molecular formula: C27H28Cl2N4O4S. Mole weight: 575.51. | |
| CS-7017 monohydrate | CS-7017 monohydrate is a peroxisome proliferator activated receptor gamma (PPAR) agonist. It is a potential therapy for thyroid cancer and liposarcoma. It is also used for the treatment of rectal cancer and non-small cell lung cancer. It was developed by Daiichi Sankyo Company Limited. It is in clinic phase 2 with no progress. Uses: Cs-7017 monohydrate is a potential therapy for thyroid cancer and liposarcoma. it is also used for the treatment of rectal cancer and non-small cell lung cancer. Synonyms: CS-7017 monohydrate; CS 7017 monohydrate; CS7017 monohydrate; Efatutazone dihydrochloride monohydrate;5-[[4-[[6-(4-Amino-3,5-dimethylphenoxy)-1-methylbenzimidazol-2-yl]methoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione hydrate dihydrochloride;Inolitazone dihydrochloride monohydrate;(+/-)-2,4-Thiazolidinedione, 5-((4-((6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl)methoxy)phenyl)methyl)-, dihydrochloride, monohydrate. Grades: >99 %. CAS No. 1048002-36-3. Molecular formula: C27H30Cl2N4O5S. Mole weight: 593.52. | |
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