Inhibitor of the multidrug transporter BCRP
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Ko 143

Item No. 15215

Technical Information
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
Purity
≥98%
Formulation
A crystalline solid
DMF: 25 mg/mlDMSO: 20 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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).1 It is much less effective at the transporters P-glycoprotein and multidrug resistance-associated protein 1, MRP1.1 Ko 143 is effective in vivo in mice.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Allen, J.D., van Loevezijn, A., Lakhai, J.M., et alPotent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol. Cancer Ther. 1(6), 417-425 (2002).

    2. Wanek, T., Kuntner, C., Bankstahl, J.P., et alA novel PET protocol for visualization of breast cancer resistance protein function at the blood-brain barrier. J. Cereb. Blood Flow Metab. 32(11), 2002-2011 (2012).