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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
KS176 is a novel potent and highly selective/specific inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter with IC50 values of 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively. It displays no inhibitory activity against P-gp or MRP1. KS176 and its analogs share a noncompetitive-type interaction with pheophorbide A. Experiments with imatinib and pheophorbide A revealed a mixed-type interaction. This class of specific breast cancer resistance protein (BCRP) inhibitors showed no inhibition of the ATP binding cassette (ABC) transporters P-gp and MRP1. Some of these modulators inhibit BCRP with high potency; they are only slightly less potent than Ko143 and could serve as promising lead structures for the design of novel effective BCRP inhibitors. These inhibitors are structurally related to tariquidar (XR9576) and belong to a library of multidrug-resistance modulators
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ln Vivo |
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Animal Protocol |
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References |
ChemMedChem.2010 Sep 3;5(9):1498-505.
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Molecular Formula |
C22H19N3O5
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Molecular Weight |
405.4
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CAS # |
1253452-78-6
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Related CAS # |
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SMILES |
O=C(C1=C(NC(C2=CC=C([N+]([O-])=O)C=C2)=O)C=CC=C1)NC3=CC=C(CCO)C=C3
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4667 mL | 12.3335 mL | 24.6670 mL | |
5 mM | 0.4933 mL | 2.4667 mL | 4.9334 mL | |
10 mM | 0.2467 mL | 1.2333 mL | 2.4667 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.