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Ko 143

Product Name
Ko 143
CAS No.
461054-93-3
Chemical Name
Ko 143
Synonyms
Ko 143;12aS)-;4-dioxo-;6]pyrido[3;Ko143 ,99%;Pyrazino[1';Ko143 hydrate;KO 143;KO-143;KO143;Ko-143, BCRP inhibitor;4-b]indole-3-propanoicacid
CBNumber
CB81562442
Molecular Formula
C26H35N3O5
Formula Weight
469.57
MOL File
461054-93-3.mol
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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
form 
powder
pka
13.31±0.60(Predicted)
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.
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Safety

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26-36
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
K2144
Product name
Ko143 hydrate
Purity
≥98% (HPLC)
Packaging
1mg
Price
$125
Updated
2024/03/01
Sigma-Aldrich
Product number
K2144
Product name
Ko143 hydrate
Purity
≥98% (HPLC)
Packaging
5mg
Price
$497
Updated
2024/03/01
Cayman Chemical
Product number
15215
Product name
Ko 143
Purity
≥98%
Packaging
5mg
Price
$120
Updated
2024/03/01
Cayman Chemical
Product number
15215
Product name
Ko 143
Purity
≥98%
Packaging
10mg
Price
$216
Updated
2024/03/01
Cayman Chemical
Product number
15215
Product name
Ko 143
Purity
≥98%
Packaging
25mg
Price
$448
Updated
2024/03/01
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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

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Ko 143 Suppliers

Canada 1 China 82 The Netherlands 1 United Kingdom 1 United States 16 Global 101
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
94657
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15839
Advantage
69
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Pure Chemistry Scientific Inc.
Tel
001-857-928-2050 or 1-888-588-9418
Fax
001-617-206-9595
Email
sales@chemreagents.com
Country
United States
ProdList
10186
Advantage
62
Shanghai Boc Chemical Co.,Ltd
Tel
021-34975603-808 18721111801
Fax
+86-21-34975602-805
Email
sales@bocpharma.com
Country
China
ProdList
997
Advantage
64
Chemsky（shanghai）International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@163.com
Country
China
ProdList
283
Advantage
58
Chemsky (shanghai) International Co.,Ltd
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
15402
Advantage
60
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
14055
Advantage
65
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-400-6206333 18521732826
Fax
021-50323701
Email
market@aladdin-e.com
Country
China
ProdList
25003
Advantage
65
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View Lastest Price from Ko 143 manufacturers

Career Henan Chemical Co
Product
Ko 143 461054-93-3
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2020-01-01

461054-93-3, Ko 143Related Search:

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  • 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)
  • Ko 143
  • (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
  • 12a-octahydro-9-Methoxy-6-(2-Methylpropyl)-1
  • 12aS)-
  • 4-b]indole-3-propanoicacid
  • 4-dioxo-
  • 6]pyrido[3
  • Pyrazino[1'
  • Ko143 ,99%
  • (3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2'
  • Ko143 hydrate
  • tert-Butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7, 12,12a-octahydropyrazino[1
  • (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',2':1,6]pyrido[3,4-b]indol-3-yl)propanoate
  • 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
  • 1,6]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':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester
  • 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 tert-Butyl Ester
  • Ko-143, BCRP inhibitor
  • 461054-93-3
  • C26H35N3O5
  • C26H36N3O5
  • Chiral Reagents
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals