Ko 143 | Tocris Bioscience 3241 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

Ko 143

catalog :

3241

quantity :

1 mg (also 10 mg)

price :

134 USD

more info or order :

Tocris Bioscience product webpage

citations: 13

Reference
Le Coz V, Zhu C, Devocelle A, Vazquez A, Boucheix C, Azzi S, et al. IGF-1 contributes to the expansion of melanoma-initiating cells through an epithelial-mesenchymal transition process. Oncotarget. 2016;7:82511-82527 pubmed publisher
Ding R, Jin S, Pabon K, Scotto K. A role for ABCG2 beyond drug transport: Regulation of autophagy. Autophagy. 2016;12:737-51 pubmed publisher
Kumar J, Wei B, Madigan J, Simpson R, Hall M, Gottesman M. Bioluminescent imaging of ABCG2 efflux activity at the blood-placenta barrier. Sci Rep. 2016;6:20418 pubmed publisher
Morfouace M, Cheepala S, Jackson S, Fukuda Y, Patel Y, Fatima S, et al. ABCG2 Transporter Expression Impacts Group 3 Medulloblastoma Response to Chemotherapy. Cancer Res. 2015;75:3879-89 pubmed publisher
Westover D, Ling X, Lam H, Welch J, Jin C, Gongora C, et al. FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irinotecan in colon and lung cancer models with ABCG2-induced resistance. Mol Cancer. 2015;14:92 pubmed publisher
Hoque M, Kis O, De Rosa M, Bendayan R. Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters. Antimicrob Agents Chemother. 2015;59:2572-82 pubmed publisher
Moreno Sanz G, Barrera B, Armirotti A, Bertozzi S, Scarpelli R, Bandiera T, et al. Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain. Pharmacol Res. 2014;87:87-93 pubmed publisher
Moreno Sanz G, Duranti A, Melzig L, Fiorelli C, Ruda G, Colombano G, et al. Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. J Med Chem. 2013;56:5917-30 pubmed publisher
Lainey E, Sebert M, Thepot S, Scoazec M, Bouteloup C, Leroy C, et al. Erlotinib antagonizes ABC transporters in acute myeloid leukemia. Cell Cycle. 2012;11:4079-92 pubmed publisher
Hill C, Jamieson D, Thomas H, Brown C, Boddy A, Veal G. Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo. Biochem Pharmacol. 2013;85:29-37 pubmed publisher
Zander S, Sol W, Greenberger L, Zhang Y, van Tellingen O, Jonkers J, et al. EZN-2208 (PEG-SN38) overcomes ABCG2-mediated topotecan resistance in BRCA1-deficient mouse mammary tumors. PLoS ONE. 2012;7:e45248 pubmed publisher
Watson C, Dogruel M, Mihoreanu L, Begley D, Weksler B, Couraud P, et al. The transport of nifurtimox, an anti-trypanosomal drug, in an in vitro model of the human blood-brain barrier: evidence for involvement of breast cancer resistance protein. Brain Res. 2012;1436:111-21 pubmed publisher
Moreno Sanz G, Barrera B, Guijarro A, d Elia I, Otero J, Alvarez A, et al. The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system. Pharmacol Res. 2011;64:359-63 pubmed publisher

product information

brand :

Tocris

master code :

3241

SKU :

3241/1

product name :

Ko 143

description :

Potent and selective BCRP inhibitor

target :

Multidrug Transporter Inhibitors

category :

Small Molecules

unit size :

1 mg (also 10 mg)

purity :

99%

observed molecular weight :

469.57

url print :

?utm_source=distributor&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

Potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM). Displays 200-fold selectivity over P-gp and MRP-1 transporters. Increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. Inhibits ABCB1 and ABCC1 at higher concentrations. Rapidly metabolized in rat plasma.

catalog number base :

3241

product keywords :

Potent selective BCRP inhibitors inhibits MDR Breast Cancer Resistance Protein Multidrug Transporters Ko143 ATP-binding cassette Multidrug Transporters 3241,

extended description :

Potent and selective BCRP inhibitor

chemical name text :

(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

formula :

C 26 H 35 N 3 O 5

formula text :

C26H35N3O5

cas num :

461054-93-3

2020 USD :

128

2021 USD :

134 USD

storage :

Store at -20°C

more info or order :

Tocris Bioscience product webpage