NCT-505 |
| Katalog-Nr.GC33219 |
NCT-505 ist ein potenter und selektiver Inhibitor der Aldehyddehydrogenase (ALDH1A1) mit einem IC50 von 7 nM und hemmt schwach hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22,8, 20,1, >57 μM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2231079-74-4
Sample solution is provided at 25 µL, 10mM.
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NCT-505 is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22.8, 20.1, >57 μM).
NCT-505 (Compound 86) is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22.8, 20.1, >57 μM). NCT-505 has no obvious inhibitory effec on 5-hydroxyprostaglandin dehydrogenase (HPGD) and type-4 hydroxysteroid dehydrogenase (HSD17β4) (IC50, >57 μM). Moreover, NCT-505 shows potent cellular activities, reducing the viability of OV-90 cells with an EC50 of 2.10-3.92 μM. NCT-505 is also cytotoxic to SKOV-3-TR cells, with IC50s of 1, 3, 10, 20, 30 μM, respectively, in the titration assay[1].
[1]. Yang SM, et al. Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity. J Med Chem. 2018 Jun 14;61(11):4883-4903.
Cell experiment: | Cells are harvested, and an equal volume of first compound (NCT-505 or paclitaxel (Taxol)) at the indicated concentration or vehicle DMSO (final DMSO concentration is the same in all conditions) is added to the cell suspension before dispensing. Cells are dispensed into 384-well, white, TC-treated plates at a density of 3000 cells/well in a volume of 30 μL of growth media/well using a Multidrop Combi dispenser. Immediately after dispensing, the second compound (ALDH1A1 inhibitor or paclitaxel) and control solutions (92 nL) are transferred using a pintool. Plates are covered with a breathable seal and incubated for 4 days at 37°C, 5% CO2, 85% RH followed by addition of 20 μL of CellTiter-Glo. After a ∼30 min incubation at rt, samples are analyzed for luminescence intensity using a ViewLux high-throughput CCD imager equipped with clear filters. Pinned compounds are tested as 16-point dilution series, with concentrations ranging from 30.7 μM to 70.1 nM for ALDH1A1 inhibitors (NCT-505, etc.) or 31.7 μM to 0.034 nM for paclitaxel, in triplicate. Data are normalized to positive control bortezomib (1 μM final) and neutral control DMSO[1]. |
References: [1]. Yang SM, et al. Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity. J Med Chem. 2018 Jun 14;61(11):4883-4903. | |
| Cas No. | 2231079-74-4 | SDF | |
| Canonical SMILES | N#CC1(C2=CC=CC=C2)CCN(C3=C(C(N4CCN(S(=O)(C)=O)CC4)=O)C=NC5=CC=C(F)C=C35)CC1 | ||
| Formula | C27H28FN5O3S | M.Wt | 521.61 |
| Löslichkeit | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9171 mL | 9.5857 mL | 19.1714 mL |
| 5 mM | 0.3834 mL | 1.9171 mL | 3.8343 mL |
| 10 mM | 0.1917 mL | 0.9586 mL | 1.9171 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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