Polmacoxib (CG100649) 是一种首创的,具有口服活性的非甾体抗炎药 (NSAID),它是一种双重抑制剂,可以抑制COX-2(IC50~ 0.1 μg/ml)和碳酸酐酶 (carbonic anhydrase)。Polmacoxib 在小鼠模型中抑制大肠腺瘤和肿瘤生长。
生物活性 | Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor ofCOX-2(IC50around 0.1 μg/ml) andcarbonic anhydrase[1]. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models[2]. |
IC50& Target[1] | COX-2 0.1 μg/mL (IC50) | carbonic anhydrase |
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体外研究 (In Vitro) | Polmacoxib (CG100649) (0-1 μg/ml; 24 hours; HCA-7 and HT-29 cells) can inhibit COX-2 activity and PGE2 production in human colon cancer cells, at lower concentrations compared to Celecoxib[2].
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体内研究 (In Vivo) | Polmacoxib (7 mg/kg; p.o.; daily for 8 weeks) suppresses intestinal polyp formation in ApcMin/+mice[2]. Polmacoxib (7-15 mg/kg; p.o.; daily from day 27 post-injection to day 111; athymic nude mice; subcutaneous xenograft mouse model) reduces tumor volume and tumor weight by 58% and 48%, respectively, compared to a 48% and 36% reduction following treatment with Celecoxib[2]. Polmacoxib (7-15 mg/kg; p.o.; began on day 14 and continued for 8 weeks; athymicnu/numice; orthotopic xenograft mouse model) inhibits CRC growth in an orthotopic xenograft mouse model, reducing tumor weight by 70% using 7 mg/kg or by 83% using 15 mg/kg, compared to a similar 70% reduction following treatment with 500 mg/kg of Celecoxib[2].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(691.77 mM;Need ultrasonic) 配制储备液 1 mM | 2.7671 mL | 13.8355 mL | 27.6709 mL | 5 mM | 0.5534 mL | 2.7671 mL | 5.5342 mL | 10 mM | 0.2767 mL | 1.3835 mL | 2.7671 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.76 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.76 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
*以上所有助溶剂都可在本网站选购。 |