Ko 143

ChemicalBook > CAS DataBase List > 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;4-b]indole-3-propanoicacid;12a-octahydro-9-Methoxy-6-(2-Methylpropyl)-1
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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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

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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

461054-93-3

C26H35N3O5

C26H36N3O5

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