K2144

Ko143 hydrate

≥98% (HPLC), powder, BCRP inhibitor

• Synonyme(s) : (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
• Formule empirique (notation de Hill): C₂₆H₃₅N₃O₅ · xH₂O
• Numéro CAS: 461054-93-3
• Poids moléculaire : 469.57 (anhydrous basis)
• Numéro MDL: MFCD19053160
• Code UNSPSC : 12352200
• ID de substance PubChem : 329817134
• Nomenclature NACRES : NA.77

Propriétés

• product name: Ko143 hydrate, ≥98% (HPLC)
• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: white to off-white
• Solubilité: DMSO: >10 mg/mL
• Auteur: GlaxoSmithKline
• Température de stockage: room temp
• Chaîne SMILES: 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
• 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
• Clé InChI: ZXXZDXPNJJZRDC-PSLBYKFTSA-N

Description

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

Actions biochimiques/physiologiques

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.

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.

Caractéristiques et avantages

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.

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Stockage et stabilité

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.

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H315,H319,H335
• Conseils de prudence: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Classification des risques: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Organes cibles: Respiratory system
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable