Mavacoxib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Mavacoxib 是一种选择性环氧合酶-2 (COX-2) 抑制剂，具有抗肿瘤活性。

Mavacoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) with?Anti-Tumour activity.

Mavacoxib (0-200 μM; 72 hours; CSKOS, U2OS, REM, K9TCC and T24 cells) treatment reduces cell viability in a dose-dependent manner. However, sensitivity to Mavacoxib varied between the cell lines, with IC50 values ranging from 34.5 μM to 157.7 μM. The IC50 values of U2OS, KTOSA5, CSKOS, REM, LILY, K9TCC, K9TCC-AXA, K9TCC-In, K9TCC-Sh, T24, 5637 and HT-1376 cells are 52.6 μM, 89.8 μM, 106.3 μM, 66.6 μM, 97.5 μM, 54.9 μM, 34.5 μM, 78.7 μM, 50.7 μM, 63.4 μM, 72.5 μM and 157.7 μM, respectively.Mavacoxib (0-200 μM; 48 hours; KTOSA5, REM, LILY, K9TCC, U2OS, and T24 cells) treatment can induce caspase-dependent apoptosis in a number of cell lines.Mavacoxib (0-75 μM; 24 hours; CSKOS, U2OS, REM, K9TCC and T24 cells) treatment down-regulates tCell Viability Assay Cell Line:CSKOS, U2OS, REM, K9TCC and T24 cells Concentration:0 μM, 0.04 μM, 25 μM, 50 μM, 75 μM, 100 μM, 125 μM, 150 μM, 175 μM, 200 μMIncubation Time:72 hoursResult:Cell viability was reduced in a dose-dependent manner.Apoptosis Analysis Cell Line:KTOSA5, REM, LILY, K9TCC, U2OS, and T24 cells Concentration:0 μM, 50 μM, 100 μM, 200 μMIncubation Time:48 hours Result:Induced apoptosis in canine and human cancer cell lines.Cell Viability Assay Cell Line:CSKOS, U2OS, REM, K9TCC and T24 cells Concentration:0 μM, 25 μM, 50 μM or 75 μM Incubation Time:24 hours Result:In CSKOS cells, p-Akt was downregulated, as was total Akt in U2OS cells. In REM cells, both p-ERK and p-Akt were increased in expression, and in K9TCC cells p-ERK expression was also increased.

Osteoarthritic dogs enrolled in the studies are randomized to receive treatment with Mavacoxib and daily placebo for carprofen or placebo for Mavacoxib and daily carprofen at a nominal dose of 4 mg/kg BW. Mavacoxib is administered in both studies with a 2-week interval between the first and second doses but with monthly dosing thereafter. The nominal Mavacoxib doses in Studies 1 and 2 are 4 and 2 mg/kg BW, respectively. Seven Mavacoxib doses are administered in Study 1, but only five doses in Study 2. In Study 1, Mavacoxib is administered without regard to the timing of meals, but in Study 2, all of the Mavacoxib doses are administered with food.

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Chromatin/Epigenetic

COX

COX-2

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170569-88-7

385.34

C16H11F4N3O2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (259.51 mM)

NS(=O)(=O)c1ccc(-n2nc(C(F)(F)F)cc2-c2ccc(F)cc2)cc1

4-(5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years