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Tak 243 mln7243

Manufactured by Chemietek

TAK-243 (MLN7243) is a small molecule laboratory reagent. It functions as a specific and potent inhibitor of the enzyme NEDD8-activating enzyme (NAE). The core function of TAK-243 is to disrupt the NEDD8 conjugation pathway, which is involved in the regulation of various cellular processes.

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3 protocols using tak 243 mln7243

1

Evaluating TAK-243 and Rapamycin in Xenograft Mouse Model

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Tumor fragments from stable TG lines were implanted subcutaneously in ~4–6 week-old NOD/SCID mice. When tumor volumes reached ~300 mm3, mice were allocated into different treatment groups as previously described (Sivanand et al., 2012 ; Pavía-Jiménez et al., 2014). TAK-243 (MLN7243) (Chemietek) was administered IV every 72 hours at 25 mg/kg in 20% 2-hydroxypropyl-β-cyclodextrin (HPβCD). Rapamycin (positive control) was administered intraperitoneally at 0.5 mg/kg in 5% ethanol, 5% PEG400, 5% Tween 80, and 85% D5W every 48 hours. Mouse weight and tumor volumes were typically assessed three times per week. Tumor volume was measured using calipers and calculated as previously reported (Pavía-Jiménez et al., 2014 (link)). Data are reported as tumor means ± SD.
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2

TAK-243 and Immunoblotting Protocol

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TAK-243 (MLN 7243) was purchased from Chemietek (CT-M7243) for in vitro and in vivo studies. The antibodies used in this study were purchased from Cell Signaling and Santa Cruz. All primary antibodies were used at 1:1000 dilutions. Corresponding HRP-conjugated secondary antibodies were used at 1:5000 dilution.
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3

Evaluating TAK-243 and Rapamycin in Xenograft Mouse Model

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Tumor fragments from stable TG lines were implanted subcutaneously in ~4–6 week-old NOD/SCID mice. When tumor volumes reached ~300 mm3, mice were allocated into different treatment groups as previously described (Sivanand et al., 2012 ; Pavía-Jiménez et al., 2014). TAK-243 (MLN7243) (Chemietek) was administered IV every 72 hours at 25 mg/kg in 20% 2-hydroxypropyl-β-cyclodextrin (HPβCD). Rapamycin (positive control) was administered intraperitoneally at 0.5 mg/kg in 5% ethanol, 5% PEG400, 5% Tween 80, and 85% D5W every 48 hours. Mouse weight and tumor volumes were typically assessed three times per week. Tumor volume was measured using calipers and calculated as previously reported (Pavía-Jiménez et al., 2014 (link)). Data are reported as tumor means ± SD.
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