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Ko143 hydrate

SIGMA/K2144 - ≥98% (HPLC)

Synonym: (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; Ko-143 hydrate

CAS Number: 461054-93-3 (anhydrous)
Empirical Formula (Hill Notation): C26H35N3O5 · xH2O
Molecular Weight: 469.57 (anhydrous basis)
MDL Number: MFCD19053160
Linear Formula: C26H35N3O5 · xH2O
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-K2144-1MG 1 mg
 $139.00
1/EA		 Add To Favorites
45-K2144-5MG 5 mg
 $547.00
1/EA		 Add To Favorites
This picture is provided solely for illustration purposes. Optical properties of the actual product may deviate. Relevant product information is printed on labeled products and other accompanying or available information material. This image depicts SKU: K2144-1MG
This picture is provided solely for illustration purposes. Optical properties of the actual product may deviate. Relevant product information is printed on labeled products and other accompanying or available information material. This image depicts SKU: K2144-5MG

 

assay ≥98% (HPLC)
color white to off-white
form powder
InChI 1S/C26H35N3O5.H2O/c1-14(2)11-20-23-17(16-8-7-15(33-6)12-19(16)27-23)13-21-24(31)28-18(25(32)29(20)21)9-10-22(30)34-26(3,4)5;/h7-8,12,14,18,20-21,27H,9-11,13H2,1-6H3,(H,28,31);1H2/t18-,20-,21-;/m0./s1
InChI key ZXXZDXPNJJZRDC-PSLBYKFTSA-N
originator GlaxoSmithKline
Quality Level 100 
SMILES string O.COc1ccc2c3C[C@@H]4N([C@@H](CC(C)C)c3[nH]c2c1)C(=O)[C@H](CCC(=O)OC(C)(C)C)NC4=O
solubility DMSO: >10 mg/mL
storage temp. room temp
Application: 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
Biochem/physiol Actions: Ko143 has been used as a positive control inhibitor on functions of BCRP in MCF7 and BCRP over-expressing MCF7/MX100 cell lines using a BCRP prototypical substrate mitoxantrone.
Biochem/physiol Actions: Ko143 has been used as a positive control inhibitor on functions of BCRP in MCF7 and BCRP over-expressing MCF7/MX100 cell lines using a BCRP prototypical substrate mitoxantrone. The ABCG2 transporter breast cancer resistance protein (BCRP) plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. It increases intracellular drug accumulation and reverse BCRP-mediated multidrug resistance. It blocked topotecan and ABZSO transport in a concentration-dependent manner. Ko143 is reported to be a more specific inhibitor of BCRP than other known inhibitors of BCRP such as fumitremorgin C and GF120918.
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.
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.
Features and Benefits: This compound is a featured product for ADME Tox research. Click here  to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm .
Features and Benefits: This compound was developed by GlaxoSmithKline . To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here .
Packaging: 1, 5 mg in glass bottle
Preparation Note: The stability of this product in solution has not been determined. According to various sources this product can be stored in solvent (DMSO) at -80°C for 6 months and -20°C for 1 month.
Purity ≥98% (HPLC)
Storage Temp. room temp
UNSPSC 12352200

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