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| 25mg |
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Purity: ≥98%
NVP-231 is a novel, potent, specific, and reversible CerK inhibitor that competitively inhibits binding of ceramide to CerK with IC50 of 12±2 nM. NVP-231 inhibits phosphorylation of ceramide and is active at low nanomolar concentrations on both purified and cellular CerK. This lowers the levels of endogenous C1P. NVP-231 increased ceramide levels and inhibited cell growth when used in conjunction with another ceramide metabolizing inhibitor, such as tamoxifen. To control ceramide metabolism, NVP-231 is thus a brand-new and promising substance that may shed light on CerK physiological function.
| Targets |
CerK (IC50 = 12 nM); apoptosis
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| ln Vitro |
NVP-231 causes cancer cells to die, which lowers cell viability and DNA synthesis. Cells treated with NVP-231 exhibited M phase arrest as opposed to G2/M boundary arrest. NVP-231 treatment results in a concentration-dependent up-regulation of cyclin B1 phosphorylation at Ser133 and a decrease of CDK1 phosphorylation at Tyr15 in MCF-7 and NCI-H358 cells. NVP-231 inhibits Wee1 expression in NCI-H358 and MCF-7 cells. Cancer cells treated with NVP-231 exhibit concentration- and time-dependent down-regulation of the CDK4 protein. In synchronized cells, this effect is even more pronounced[2].
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| Cell Assay |
MCF-7 and NCI-H358 cells are plated in a 96-well black plate at a density of 1 × 104 cells per well, and they are then exposed to the indicated concentrations of NVP-231 (in nM) for 48 hours. During the final 4 hours of the treatment, alamarBlueR is added, and fluorescence is measured.
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| References |
| Molecular Formula |
C25H25N3O2S
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|---|---|
| Molecular Weight |
431.5499
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| Exact Mass |
431.55
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| Elemental Analysis |
C, 69.58; H, 5.84; N, 9.74; O, 7.41; S, 7.43
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| CAS # |
362003-83-6
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| Related CAS # |
362003-83-6
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| Appearance |
White to off-white solid powder
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| SMILES |
C1C2CC3CC1CC(C2)(C3)C(=O)NC4=CC5=C(C=C4)N=C(S5)NC(=O)C6=CC=CC=C6
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| InChi Key |
MVSSJPGNLQPWSW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H25N3O2S/c29-22(18-4-2-1-3-5-18)28-24-27-20-7-6-19(11-21(20)31-24)26-23(30)25-12-15-8-16(13-25)10-17(9-15)14-25/h1-7,11,15-17H,8-10,12-14H2,(H,26,30)(H,27,28,29)
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| Chemical Name |
N-(2-benzamido-1,3-benzothiazol-6-yl)adamantane-1-carboxamide
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| Synonyms |
NVP231; NVP 231; NVP-231
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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: ≥41 mg/mL (~95.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.79 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 (5.79 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 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 (5.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3172 mL | 11.5861 mL | 23.1723 mL | |
| 5 mM | 0.4634 mL | 2.3172 mL | 4.6345 mL | |
| 10 mM | 0.2317 mL | 1.1586 mL | 2.3172 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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