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NSC625987 141992-47-4

NSC625987 141992-47-4

CAS No.: 141992-47-4

NSC 625987 is a specific, high-affinity CDK4 inhibitor (antagonist) with IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987
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This product is for research use only, not for human use. We do not sell to patients.

NSC 625987 is a specific, high-affinity CDK4 inhibitor (antagonist) with IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 is more than 500 times more selective for CDK4 than CDK2.

Physicochemical Properties


Molecular Formula C15H13NO2S
Molecular Weight 271.334
Exact Mass 271.067
CAS # 141992-47-4
PubChem CID 3004085
Appearance Brown to khaki solid powder
Density 1.32g/cm3
Boiling Point 460.4ºC at 760 mmHg
Flash Point 232.2ºC
Vapour Pressure 1.17E-08mmHg at 25°C
Index of Refraction 1.683
LogP 4.067
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 2
Heavy Atom Count 19
Complexity 349
Defined Atom Stereocenter Count 0
InChi Key KFAKESMKRPNZTM-UHFFFAOYSA-N
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)
Chemical Name

1,4-dimethoxy-10H-acridine-9-thione
Synonyms

NSC625987; NSC-625987; NSC 625987
HS Tariff Code 2934.99.9001
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)

Biological Activity


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].
References

[1]. The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4. Clin Cancer Res. 1999 Dec;5(12):4279-86.

[2]. Natriuretic peptide receptor-C agonist attenuates the expression of cell cycle proteins and proliferation of vascular smooth muscle cells from spontaneously hypertensive rats: role of Gi proteins and MAPkinase/PI3kinase signali.

Additional Infomation 1,4-dimethoxy-10H-acridine-9-thione is a member of acridines.

Solubility Data


Solubility (In Vitro) DMSO : ~100 mg/mL (~368.55 mM)
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.