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NVS-CECR2-1 is a novel and potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2) with an IC 50 of 47 nM. CECR2 (cat eye syndrome chromosome region, candidate 2) gene previously was identified as being in the chromosome 22q11 region, duplicated in the human disorder cat eye syndrome.
| ln Vitro |
NVS-CECR2-1 diminishes all pancreatic viability at 1-4 μM for 72 hours [1]. NVS-CECR2-1 (1-6 μM; 72 hours) was developed to boost mitochondria within cells [1]. In SW48 cells, NVS-CECR2-1 (10 μM; 2 hr) suppresses CECR2 BRD's chromatin binding. Its IC50 value is predicted to be 0.64 μM. NVS-CECR2-1 (0.5–4 μM; 10 days) decreases the clonogenic activity of SW48 cells in a dose-dependent manner. NVS-CECR2-1 (5, 10, 15 μM; 2 hours) cleaves chromatin from chromatin in a linear manner. a distance from CECR2 that doesn't impact BRG1[1]. -CECR2-1 removes CECR2 from intracellular chromatin and prevents the CECR2 BRD from binding to chromatin [1].
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| Cell Assay |
Cell viability assay[1]
Cell Types: colon (SW48, HT29 and HCT116), lung (H460), urinary epithelium (SV-HUC-1), cervix (HeLa) and bone (U2OS), human embryonic kidney (HEK) 293 T cell Tested Concentrations: 1, 1.5, 2, 2.5, 3, 4 μM Incubation Duration: 72 hrs (hours) Experimental Results: Viability diminished in all cancer cells analyzed in a dose-dependent manner. demonstrated dose-dependent cytotoxicity against HEK 293 T cells. Apoptosis analysis [1] Cell Types: SW48 cells Tested Concentrations: 0.5, 1, 1.5, 2, 4, 6 μM Incubation Duration: 72 hrs (hours) Experimental Results: Apoptosis increased in a dose-dependent manner, exceeding 80% of cells at 6°C Apoptosis occurs at μM and has little effect on necrosis. |
| References |
| Molecular Formula |
C27H37N5O2S
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|---|---|
| Molecular Weight |
495.68
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| Exact Mass |
495.266
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| CAS # |
1992047-61-6
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| Related CAS # |
1992047-61-6;NVS-CECR2-1 HCl;
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| PubChem CID |
117072550
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
712.7±70.0 °C at 760 mmHg
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| Flash Point |
384.8±35.7 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.659
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| LogP |
4.14
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
836
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XVECNLUKQDKOST-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H37N5O2S/c1-6-13-35(33,34)25-29-22(15-24(30-25)28-20-8-9-20)18-7-10-23-19(14-18)11-12-32(23)21-16-26(2,3)31-27(4,5)17-21/h7,10-12,14-15,20-21,31H,6,8-9,13,16-17H2,1-5H3,(H,28,29,30)
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| Chemical Name |
N-cyclopropyl-2-propylsulfonyl-6-[1-(2,2,6,6-tetramethylpiperidin-4-yl)indol-5-yl]pyrimidin-4-amine
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| Synonyms |
NVSCECR21 NVS1NVS CECR2 1 NVS-1 NVS 1 NVS-CECR2-1
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~66.67 mg/mL (~134.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0174 mL | 10.0872 mL | 20.1743 mL | |
| 5 mM | 0.4035 mL | 2.0174 mL | 4.0349 mL | |
| 10 mM | 0.2017 mL | 1.0087 mL | 2.0174 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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