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Ko-143 (Ko143) is a novel and potent breast cancer resistance protein multidrug transporter (BCRP) inhibitor, or an ATP-binding cassette sub-family G member 2 (ABCG2) inhibitor.
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| ln Vitro |
Ko143 (10 nM) dramatically lowers the IC50 of MTX on mouse G2 and HEK G2 cells by a factor of 2.5. ABC transporter function is not inhibited by Ko143 (1-100 μM) metabolites [1]. Ko143, an FTC analog, overcomes drug resistance in human IGROV1/T8 cells and mouse MEF3.8/T6400 cells chosen with SKF 104864A. At zero, one, or eight times the EC90 of 25 nM, Ko143 can be utilized [2]. In Madin-Darby canine kidney (MDCK) 2-BCRP421CC (wild-type) and MDCK2-BCRP421AA (mutant) cells, Ko143 inhibits BCRP-mediated ZD 4522 trafficking [3].
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| ln Vivo |
In mice, Ko143 (10 mg/kg, po) raises SKF 104864A's oral availability [2]. Ko143 has a major impact on ZD 4522's pharmacokinetics in rats [3].
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| Cell Assay |
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| References | ||
| Additional Infomation |
LSM-6260 is a member of beta-carbolines and a tert-butyl ester.
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| Molecular Formula |
C26H35N3O5
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|---|---|
| Molecular Weight |
469.582
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| Exact Mass |
469.257
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| CAS # |
461054-93-3
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| PubChem CID |
10322450
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
689.8±55.0 °C at 760 mmHg
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| Melting Point |
147ºC
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| Flash Point |
371.0±31.5 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.597
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| LogP |
2.42
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
34
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| Complexity |
794
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC(C)C[C@H]1C2=C(C[C@@H]3N1C(=O)[C@@H](NC3=O)CCC(=O)OC(C)(C)C)C4=C(N2)C=C(C=C4)OC
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| InChi Key |
NXNRAECHCJZNRF-JBACZVJFSA-N
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| 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
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| Chemical Name |
tert-butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1',2'
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| Synonyms |
Ko-143 Ko-143 Ko-143
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~100 mg/mL (~212.96 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.32 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication (<50°C). For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.5 mg/mL (5.32 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1296 mL | 10.6478 mL | 21.2956 mL | |
| 5 mM | 0.4259 mL | 2.1296 mL | 4.2591 mL | |
| 10 mM | 0.2130 mL | 1.0648 mL | 2.1296 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.
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