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| Targets |
NSC625987 targets the cyclin-dependent kinase 4 (CDK4) in complex with cyclin D1. CDK4 is a key regulator of the cell cycle, controlling the transition from G1 to S phase. By inhibiting CDK4 activity, NSC625987 prevents the phosphorylation of the retinoblastoma protein (Rb), leading to cell cycle arrest.
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| ln Vitro |
In spontaneously hypertensive rats (SHR) rats, NSC 625987 (10 nM, 50 nM, and 100 nM) therapy reduced the increased proliferation of vascular smooth muscle cells (VSMC) by around 35% [2].
In vitro, NSC625987 acts as a potent and selective CDK4 inhibitor with an IC₅₀ of 0.2 µM for the Cdk4/cyclin D1 complex. It exhibits exceptional selectivity for CDK4, being >500-fold more selective for CDK4 over CDK2. Its in vitro activity is assessed using kinase assays that measure the phosphorylation of CDK4 substrates. |
| ln Vivo |
NSC625987 is used in research to study cell cycle regulation and p16-related tumors. Its in vivo activity has been studied in preclinical models of cancer, where CDK4 inhibition leads to reduced tumor cell proliferation. The compound serves as a tool for investigating the role of CDK4 in tumorigenesis and for developing CDK4-based anticancer therapies.
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| Enzyme Assay |
The in vitro enzyme assay for NSC625987 involves measuring its inhibitory activity against CDK4/cyclin D1 in cell-free systems. These assays use purified CDK4/cyclin D1 enzyme complexes and measure the phosphorylation of a substrate peptide in the presence of the compound. Inhibitory potency is determined by assessing the IC₅₀ (0.2 µM). Selectivity over CDK2 and CDK1 is also assessed.
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| Cell Assay |
In vitro cellular assays for NSC625987 are performed using cancer cell lines that are dependent on CDK4 activity for proliferation. These assays measure the compound's ability to inhibit cell cycle progression, induce G1 arrest, and reduce cell viability. The compound's effects on Rb phosphorylation are also assessed by Western blotting.
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| Animal Protocol |
In vivo animal studies for NSC625987 are conducted in mouse xenograft models of CDK4-dependent tumors. These studies typically involve administration of the compound, followed by assessment of tumor growth inhibition, cell cycle markers, and survival. The compound's efficacy and selectivity for CDK4 over CDK2 are evaluated in these models.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NSC625987 are characterized by its molecular properties: molecular formula C₁₉H₁₈N₄O₂ and molecular weight 334.37 g/mol. The compound is soluble in DMSO and is typically administered in preclinical studies via intraperitoneal or oral routes. Its pharmacokinetic profile supports its use in cancer research.
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| Toxicity/Toxicokinetics |
Toxicology studies of NSC625987 have been conducted to support its use in preclinical research. As a CDK4 inhibitor, its toxicology profile includes effects on rapidly dividing cells, such as bone marrow and gastrointestinal epithelial cells. The compound's selectivity for CDK4 over CDK2 may contribute to an improved safety profile.
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| References |
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| Additional Infomation |
1,4-Dimethoxy-10H-acridin-9-thione is a member of the acridine class of compounds.
NSC625987 (CAS: 141992-47-4) is a potent and selective CDK4 inhibitor with an IC₅₀ of 0.2 µM for the Cdk4/cyclin D1 complex. It exhibits >500-fold selectivity for CDK4 over CDK2, with IC₅₀ values >100 µM for Cdk2/cyclin A, Cdk2/cyclin E, and Cdk1/cyclin A complexes. The compound is used to study p16-related tumors and cell cycle regulation. It is for research use only. |
| Molecular Formula |
C15H13NO2S
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|---|---|
| Molecular Weight |
271.334
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| Exact Mass |
271.067
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| CAS # |
141992-47-4
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| PubChem CID |
3004085
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| Appearance |
Brown to khaki solid powder
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| Density |
1.32g/cm3
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| Boiling Point |
460.4ºC at 760 mmHg
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| Flash Point |
232.2ºC
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| Vapour Pressure |
1.17E-08mmHg at 25°C
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| Index of Refraction |
1.683
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| LogP |
4.067
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
349
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KFAKESMKRPNZTM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H13NO2S/c1-17-11-7-8-12(18-2)14-13(11)15(19)9-5-3-4-6-10(9)16-14/h3-8H,1-2H3,(H,16,19)
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| Chemical Name |
1,4-dimethoxy-10H-acridine-9-thione
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| Synonyms |
NSC625987; NSC-625987; NSC 625987
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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 : ~100 mg/mL (~368.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.21 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 (9.21 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. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6855 mL | 18.4277 mL | 36.8555 mL | |
| 5 mM | 0.7371 mL | 3.6855 mL | 7.3711 mL | |
| 10 mM | 0.3686 mL | 1.8428 mL | 3.6855 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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