ChemicalBook > CAS DataBase List > Ko 143

Ko 143

Ko 143 Structure
Ko 143
  • CAS No.461054-93-3
  • Chemical Name:Ko 143
  • CBNumber:CB81562442
  • Molecular Formula:C26H35N3O5
  • Formula Weight:469.57
  • MOL File:461054-93-3.mol
Ko 143 Property
  • Melting point 147 ºC
  • Boiling point 689.8±55.0 °C(Predicted)
  • Density 1.24
  • storage temp. Desiccate at -20°C
  • solubility DMSO: >10mg/mL
  • pka 13.31±0.60(Predicted)
  • form powder
  • color white to off-white
  • Stability Stable for 2 years from date of purchase as supplied. Protect from exposure to moisture. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
  • UNSPSC Code 12352200
  • NACRES NA.77
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H315-H319-H335
  • Precautionary statements P261-P305+P351+P338
Ko 143 Price More Price(2)
  • Brand: Sigma-Aldrich(India)
  • Product number: K2144
  • Product name : Ko143 hydrate
  • Purity: ≥98% (HPLC)
  • Packaging: 1MG
  • Price: ₹12697.73
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: K2144
  • Product name : Ko143 hydrate
  • Purity: ≥98% (HPLC)
  • Packaging: 5MG
  • Price: ₹50379.55
  • Updated: 2022/06/14
  • Buy: Buy

Ko 143 Chemical Properties,Usage,Production

  • Description Breast cancer resistance protein (BCRP) is an ATP-binding cassette protein known also as ABCG2. While it normally functions as a high-capacity urate exporter in the renal system, it also acts as a xenobiotic transporter and contributes to multidrug resistance (e.g., to mitoxantrone) in certain types of cancer. BCRP is abundant at the intestinal epithelium and blood-brain barrier, potentially restricting the distribution of certain drugs. Ko 143 is a potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively). It is much less effective at the transporters P-glycoprotein and multidrug resistance-associated protein 1, MRP1. Ko 143 is effective in vivo in mice.
  • Uses A potent BCRP (breast cancer resistance protein) inhibitor
  • Uses Ko143 hydrate has been used:
    • to determine the role of ATP-binding cassette sub-family G member 2 (ABCG2), human embryonic kidney (HEK)-C1 and HEK-ABCG2 in tumor microenvironment
    • to inhibit ABCG2 for sphere formation assay
    • in calcein-AM efflux inhibition to monitor multidrug resistance protein (MRP)-function in kidney
    • for cell viability assay

  • Definition ChEBI: LSM-6260 is a member of beta-carbolines and a tert-butyl ester.
  • Biological Activity Potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC 90 = 26 nM). Displays > 200-fold selectivity over P-gp and MRP-1 transporters. Increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance.
  • Biochem/physiol Actions Ko143 has been used as a positive control inhibitor on functions of breast cancer resistance protein (BCRP) using a BCRP prototypical substrate mitoxantrone. BCRP, an ABCG2 transporter, plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters and thus is more specific than other known BCRP inhibitors such as fumitremorgin C and GF120918. It increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. It blocks topotecan and ABZSO transport in a concentration-dependent manner.
  • storage Store at -20°C
  • References 1) 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 2) Weidner et al. (2015), The Inhibitor Ko143 Is Not Specific for ABCG2; J. Pharmacol. Exp. Ther., 354 384 3) Palasuberniam et al. (2015), ABCG2 transporter inhibitor restores the sensitivity of triple negative breast cancer cells to aminolevulinic acid-mediated photodynamic therapy; Sci. Rep., 5 13298 4) 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 5) Sabnis et al. (2017),?The Efflux Transporter ABCG2 Maintains Prostate Stem Cells;? Mol. Cancer Res., 15 128
Ko 143 Preparation Products And Raw materials
Raw materials
Preparation Products
Ko 143 Suppliers
Global(111)Suppliers
  • Supplier：
    career henan chemical co
  • Tel：+86-0371-86658258<br/>+8613203830695
  • Email：factory@coreychem.com
  • Country：China
  • ProdList：29808
  • Advantage：58
  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：
  • Email：support@targetmol.com
  • Country：United States
  • ProdList：38630
  • Advantage：58
  • Supplier：
    Aladdin Scientific
  • Tel：
  • Email：tp@aladdinsci.com
  • Country：United States
  • ProdList：57505
  • Advantage：58
  • Supplier：
    Chongqing Chemdad Co., Ltd
  • Tel：+86-023-6139-8061<br/>+86-86-13650506873
  • Email：sales@chemdad.com
  • Country：China
  • ProdList：39927
  • Advantage：58
Ko 143 Spectrum
461054-93-3, Ko 143Related Search:
  • Intermediates & Fine Chemicals
  • Inhibitors
  • Heterocycles
  • Chiral Reagents
  • Pharmaceuticals
  • 杂质对照品
  • 抑制剂
  • 合成有机化合物配体
  • 细胞生物学试剂
  • 细胞生物学
  • 细胞信号和神经生物学
  • C26H36N3O5
  • C26H35N3O5
  • 化合物KO 143,10 MM DMSO 溶液
  • KO 143抑制剂
  • 3-((3S,6S,12AS)-6-异丁基-9-甲氧基-1,4-二氧代-1,2,3,4,6,7,12,12A-八氢吡嗪并[1',2':1,6]吡啶并[3,4-B]吲哚-3-基)丙酸叔丁酯
  • KO 143,BCRP抑制剂
  • KO143HYDRATE>=98%(HPLC)
  • KO 143 水合物
  • 乳腺癌耐药蛋白抑制剂(BCRP抑制剂)
  • 1,6]吡啶并[3,4-B]吲哚-3-丙酸叔丁酯]
  • [(3S,6S,12AS)-1,2,3,4,6,7,12,12A-八氢-9-甲氧基-6-(2-甲基丙基)-1,4-二氧代吡嗪并[1',2'
  • (3S,6S,12AS)-八氢-9-甲氧基-6-(2-甲基丙基)-1,4-二氧吡嗪并[1',2':1,6]吡啶并[3,4-B]吲哚-3-羧酸叔丁酯
  • (3S,6S,12AS)-1,2,3,4,6,7,12,12A-八氢-9-甲氧基-6-(2-甲基丙基)-1,4-二氧代吡嗪并[1',2':1,6]吡啶并[3,4-B]吲哚-3-丙酸叔丁酯
  • 461054-93-3
  • Ko 143, 10 mM in DMSO
  • Ko-143, BCRP inhibitor
  • (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 tert-Butyl Ester
  • (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
  • 1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester
  • (3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2'
  • tert-Butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino
  • KO 143;KO-143;KO143
  • tert-butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl)propanoate
  • (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 hydrate
  • tert-Butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7, 12,12a-octahydropyrazino[1
  • Ko143 hydrate
  • Ko143 ,99%
  • Pyrazino[1'
  • 6]pyrido[3
  • 4-dioxo-
  • 4-b]indole-3-propanoicacid
  • 12aS)-
  • 12a-octahydro-9-Methoxy-6-(2-Methylpropyl)-1
  • Ko 143
  • Pyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid, 1,2,3,4,6,7,12,12a-octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxo-, 1,1-dimethylethyl ester, (3S,6S,12aS)-(Ko143)

Home

My