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说明： Potent and selective BCRP inhibitor
化学名： (3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester
纯度： ≥99% (HPLC)
生物活性 for Ko 143
Ko 143 is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM). Displays > 200-fold selectivity over P-gp and MRP-1 transporters. Increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. Inhibits ABCB1 and ABCC1 at higher concentrations. Rapidly metabolized in rat plasma.
化合物库 for Ko 143
Ko 143 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Ko 143
| 分子量 | 469.57 |
| 公式 | C26H35N3O5 |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 461054-93-3 |
| PubChem ID | 10322450 |
| InChI Key | NXNRAECHCJZNRF-JBACZVJFSA-N |
| Smiles | O=C(N[C@H]4CCC(OC(C)(C)C)=O)[C@]3([H])CC1=C([C@H](CC(C)C)N3C4=O)NC2=C1C=CC(OC)=C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Ko 143
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 23.48 | 50 | |
| ethanol | 46.96 | 100 |
制备储备液 for Ko 143
以下数据基于产品分子量 469.57。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.13 mL | 10.65 mL | 21.3 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.13 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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产品说明书 for Ko 143
参考文献 for Ko 143
参考文献是支持产品生物活性的出版物。
Allen et al (2002) Potent and specific inhibition of breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol.Cancer Ther. 1 417 PMID: 12477054
Allen et al (2003) Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etop. resistance and transport, but etop. oral availability is limited primarily by P-glycoprotein. Cancer Res. 63 1339 PMID: 12649196
Loevezijn et al (2001) Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg.Med.Chem.Letts. 11 29 PMID: 11140726
Weidner et al (2015) The inhibitor Ko143 is not specific for ABCG2. J.Pharmacol.Exp.Ther. 354 384 PMID: 26148857
If you know of a relevant reference for Ko 143, please let us know.
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关键词: Ko 143, Ko 143 supplier, Potent, selective, BCRP, inhibitors, inhibits, MDR, Breast, Cancer, Resistance, Protein, Multidrug, Transporters, Ko143, ATP-binding, cassette, 3241, Tocris Bioscience
13 篇 Ko 143 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Ko 143 的部分引用包括：
Kumar et al (2016) Bioluminescent imaging of ABCG2 efflux activity at the blood-placenta barrier. Sci Rep 6 20418 PMID: 26853103
Ding et al (2016) A role for ABCG2 beyond drug transport: Regulation of autophagy. Autophagy 12 737 PMID: 26983466
Watson et al (2012) The transport of nifurtimox, an anti-trypanosomal drug, in an in vitro model of the human blood-brain barrier: evidence for involvement of breast cancer resistance protein. Antimicrob Agents Chemother 1436 111 PMID: 22200378
Coz et al (2016) IGF-1 contributes to the expansion of melanoma-initiating cells through an epithelial-mesenchymal transition process. Oncotarget 7 82511 PMID: 27764776
Westover et al (2015) FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irino. in colon and lung cancer models with ABCG2-induced resistance. Brain Res 14 92 PMID: 25928015
Hoque et al (2015) Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters. Biochem Pharmacol 59 2572 PMID: 25691630
Moreno-Sanz et al (2014) Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain. Pharmacol Res 87 87 PMID: 24993496
Hill et al (2013) Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo. J Biol Chem 85 29 PMID: 23063411
Moreno-Sanz et al (2011) The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system. Pharmacol Res 64 359 PMID: 21767647
Morfouace et al (2015) ABCG2 Transporter Expression Impacts Group 3 Medulloblastoma Response to Chemotherapy. Cancer Res 75 3879 PMID: 26199091
Moreno-Sanz et al (2013) Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. J Med Chem 56 5917 PMID: 23822179
Zander et al (2012) EZN-2208 (PEG-SN38) overcomes ABCG2-mediated topo. resistance in BRCA1-deficient mouse mammary tumors. PLoS One 7 e45248 PMID: 23028879
Lainey et al (2012) Erlotinib antagonizes ABC transporters in acute myeloid leukemia. Cell Cycle 11 4079 PMID: 23095522
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