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| 25mg |
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Purity: ≥98%
NSC23925 2HCl (NSC23925 dihyrochloride) is a novel, potent, selective and effective P-glycoprotein (Pgp) inhibitor that is able to reverse multidrug resistance (MDR), e.g. it prevents the development of paclitaxel resistance by inhibiting the introduction of P-glycoprotein and enhancing apoptosis. NSC23925 can prevent the emergence of MDR in ovarian cancer both in vitro and in vivo. The clinical use of NSC2395 at the onset of chemotherapy may prevent the development of MDR and improve the clinical outcome of patients with ovarian cancer.
| ln Vitro |
An innovative, efficient, and selective P-glycoprotein (Pgp) inhibitor is NSC23925. After being exposed to 1 μM NSC23925 for an extended period of time, SKOV-3 cells exhibit consistent proliferation in the culture medium. In order to stop paclitaxel resistance from developing while the drug is being administered, NSC23925 directly suppresses the overexpression of Pgp[1]. In several different tumor types where Multidrug resistance 1 (MDR1) is highly expressed, NSC23925 restores chemoresistance. NSC23925 dosages between 0.5 and 1 µM usually result in the maximum reversal of MDR. While the mean concentration of NSC23925 needed for the greatest reversal of resistance in SKOV-3TR or OVCAR8TR to cytotoxic medicines is 0.5 µM to 1 µM, the IC50 for NSC23925 is 8 µM in SKOV-3/SKOV-3TR and 25 µM in OVCAR8/OVCAR8TR cell lines[2].
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| ln Vivo |
Tumors treated with NSC23925 alone or saline alone both develop more slowly over time. The anticancer activity of paclitaxel is considerably prolonged when NSC23925 is used in combination with chemotherapy[1].
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| References |
[1]. Yang X, et al. Nsc23925 prevents the development of paclitaxel resistance by inhibiting the introduction of P-glycoprotein and enhancing apoptosis. Int J Cancer. 2015 Oct 15;137(8):2029-39.
[2]. Duan Z, et al. NSC23925, identified in a high-throughput cell-based screen, reverses multidrug resistance. PLoS One. 2009 Oct 12;4(10):e7415 |
| Molecular Formula |
C22H26CL2N2O2
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|---|---|
| Molecular Weight |
421.360044002533
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| CAS # |
858474-14-3
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| SMILES |
OC(C1NCCCC1)C2=CC(C3=CC=C(OC)C=C3)=NC4=CC=CC=C24.[H]Cl.[H]Cl
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| InChi Key |
WGWOQHWZXLGPNG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H24N2O2.2ClH/c1-26-16-11-9-15(10-12-16)21-14-18(17-6-2-3-7-19(17)24-21)22(25)20-8-4-5-13-23-20;;/h2-3,6-7,9-12,14,20,22-23,25H,4-5,8,13H2,1H3;2*1H
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| Chemical Name |
2-(p-Methoxyphenyl)-α-2-piperidyl-4-quinolinemethanol Dihydrochloride
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| Synonyms |
NSC 23925; NSC23925 dihyrochloride; NSC-23925; NSC 23925 diHCl
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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 : ~14.29 mg/mL (~33.91 mM)
H2O : ~4 mg/mL (~9.49 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (3.39 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 14.3 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: ≥ 1.43 mg/mL (3.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 14.3 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3733 mL | 11.8663 mL | 23.7327 mL | |
| 5 mM | 0.4747 mL | 2.3733 mL | 4.7465 mL | |
| 10 mM | 0.2373 mL | 1.1866 mL | 2.3733 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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