Ko 143

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.Formal Name: (3S,6S,12aS)-1,2,3,4,6,7,12,12a-octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxo-pyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester. CAS Number: 461054-93-3. Molecular Formula: C26H35N3O5. Formula Weight: 469.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 20 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 224, 266, 297 nm. SMILES: COC(C=C1)=CC2=C1C3=C(N2)[C@H](CC(C)C)N([C@@]4([H])C3)C([C@H](CCC(OC(C)(C)C)=O)NC4=O)=O. InChi Code: InChI=1S/C26H35N3O5/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)/t18-,20-,21-/m0/s1. InChi Key: NXNRAECHCJZNRF-JBACZVJFSA-N.