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| Cas No.: | 1190221-43-2 |
| Chemical Name: | TM 5441,TM-5441 |
| Synonyms: | TM 5441,TM-5441 |
| SMILES: | C1=CC(=CC(=C1)NC(=O)COCC(=O)NC2=C(C=C(C=C2)Cl)C(=O)O)C3=COC=C3 |
| Formula: | C21H17ClN2O6 |
| M.Wt: | 428.82 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | TM5441 is a plasminogen activator inhibitor-1 (PAI-1); inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM. |
| In Vivo: | Oral administration of TM5441 (20 mg/kg daily) to HT1080 and HCT116 xenotransplanted mice increases tumor cell apoptosis and has a significant disruptive effect on the tumor vasculature that is associated with a decrease in tumor growth and an increase in survival. The average peak plasma concentration is 11.4 μM one hour after oral administration and undetectable levels 23 hours after administration[1]. TM5441 effectively inhibits albuminuria, mesangial expansion, ECM accumulation, and macrophage infiltration in diabetic kidneys[2]. |
| In Vitro: | TM5441 dose-dependently decreases HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells with an IC50 ranging between 9.7 and 60.3 μM. TM5441 decreases tumor cell viability in part through diminished proliferation. TM5441 increases caspase 3/7 activity for both HT1080 and HCT116 cells in a dose dependant manner. TM5441is a potent stimulators of intrinsic apoptosis in tumor cells. TM5441 induces mitochondrial depolarization[1]. In mouse proximal tubular epithelial cells, TM5441 effectively inhibits PAI-1-induced mRNA expression of fibrosis and inflammation markers and also reverses PAI-1-induced inhibition of plasmin activity[2]. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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