Product Introduction
Bioactivity


英文名: Ko 143

描述: Ko 143 有效且選擇性抑制 ATP 結(jié)合盒亞家族 G 成員 2 (ABCG2/BCRP)

細胞實驗: Cells are plated at 400 or 1000/well in 96-well plates the night before the addition of drugs. A concentration series of the drug is applied along one plate axis and left for the duration of the assay. Plates are harvested after 4-5 days while untreated wells are still subconfluent. Relative cell proliferation is quantified with CyQuant or Sybr Green I fluorescent nucleic acid stains. Assays with human cell lines are performed in the presence of 0.1 μm PSC833 to inhibit confounding P-gp activity [2].

動物實驗: Oral toxicity of FTC analogs in mice is tested by mixing 50 mg/mL stocks in DMSO 1:1 with Tween 80 (polyoxyethylene sorbitan mono-oleate) and diluting with 5% w/v glucose such that the final volume administered by oral gavage is 10 μL/g of body weight. Pairs of mice are administered oral doses of 50 mg/kg Ko132, Ko134, Ko143, or vehicle under light methoxyflurane anesthesia. Final tests of 50 mg/kg Ko134 or Ko143 are performed on additional pairs of unanesthetized animals to observe any behavioral effects. Further, another pair of mice receive a higher dose of 100 mg/kg Ko134. For i.p. toxicity tests, the FTC analog stocks in DMSO are dispersed in at least 10 volumes of sterile corn oil such that the injected volume is 5 μL/g of body weight. After pilot tests at lower doses show no adverse effects, mice (4 per group) are administered vehicle or 10 mg/kg i.p. of Ko132, Ko134, or Ko143. The mice are observed continuously during the first hour after administration and then at increasing intervals for 2 weeks, after which they are sacrificed for histological examination of major organs and structures [2].

體外活性: 在HEK G2細胞和鼠標(biāo)G2細胞中，Ko143 (10 nM) 顯著降低了MTX的IC50值。Ko143 (1-100 μM) 的代謝物并不抑制ABC轉(zhuǎn)運蛋白的功能[1]。在經(jīng)SKF 104864A選育的鼠標(biāo)MEF3.8/T6400細胞和人IGROV1/T8細胞中，Ko143能夠逆轉(zhuǎn)藥物抗性[2]。Ko143抑制了在Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC（野生型）細胞和MDCK2-BCRP421AA（突變型）細胞中BCRP介導(dǎo)的ZD 4522運輸[3]。

體內(nèi)活性: Ko143（10 mg/kg，p.o.）在小鼠中提高了SKF 104864A的口服可用性[2]。

存儲條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : Insoluble
DMSO : 90 mg/mL (191.66 mM)


關(guān)鍵字: BCRP | Breast cancer resistance protein | ABCG2 | Ko-143 | Inhibitor | Ko143 | inhibit | Ko 143

相關(guān)產(chǎn)品: Triclabendazole sulfoxide | CP-100356 hydrochloride | PCI 29732 | YHO-13351 free base | Fumitremorgin C | Elacridar | Zamicastat | 6,8-Diprenylnaringenin | KS176 | YHO-13177

相關(guān)庫: Ion Channel Inhibitor Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library

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