AZD-5597Potent CDK inhibitor CAS# 924641-59-8 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 924641-59-8 | SDF | Download SDF |
| PubChem ID | 16113484 | Appearance | Powder |
| Formula | C23H28FN7O | M.Wt | 437.51 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | >15.65mg/mL in DMSO | ||
| Chemical Name | [4-[[5-fluoro-4-(2-methyl-3-propan-2-ylimidazol-4-yl)pyrimidin-2-yl]amino]phenyl]-[(3S)-3-(methylamino)pyrrolidin-1-yl]methanone | ||
| SMILES | CC1=NC=C(N1C(C)C)C2=NC(=NC=C2F)NC3=CC=C(C=C3)C(=O)N4CCC(C4)NC | ||
| Standard InChIKey | NTSDIJMNXYJJNG-SFHVURJKSA-N | ||
| Standard InChI | InChI=1S/C23H28FN7O/c1-14(2)31-15(3)26-12-20(31)21-19(24)11-27-23(29-21)28-17-7-5-16(6-8-17)22(32)30-10-9-18(13-30)25-4/h5-8,11-12,14,18,25H,9-10,13H2,1-4H3,(H,27,28,29)/t18-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
AZD-5597 Dilution Calculator
AZD-5597 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2857 mL | 11.4283 mL | 22.8566 mL | 45.7132 mL | 57.1416 mL |
| 5 mM | 0.4571 mL | 2.2857 mL | 4.5713 mL | 9.1426 mL | 11.4283 mL |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2857 mL | 4.5713 mL | 5.7142 mL |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4571 mL | 0.9143 mL | 1.1428 mL |
| 100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.4571 mL | 0.5714 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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AZD-5597 is a potent CDK inhibitor with IC50 values of 2 nM for CDK1 and CDK2, respectively [1].
The cyclin-dependent kinases (CDKs) are serine-threonine protein kinases with roles in the regulation of the cell cycle, and also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells [1].
AZD-5597 is a potent imidazole pyrimidine amide CDK inhibitor. In LoVo cells, AZD-5597 exhibited high level of anti-proliferative activity with IC50 value of 0.039 μM. AZD-5597 exhibited excellent aqueous solubility ( > 50 mg/mL), photostability (t1/2 > 24 h), hydrolytic stability (pH 4-10, t1/2 > 100 days), plasma stability ( > 18 h) and the lack of CYP inhibition. The overall profile of AZD-5597 indicated that it was suitable for further development as an iv agent [1].
In nude mouse and rat, AZD-5597 possessed good pharmacokinetic parameters with moderate to low clearance. In nude mice implanted subcutaneously with SW620 human colon adenocarcinoma cells, AZD-5597 (15 mg/kg, dosed intermittently for 3 weeks, ip) inhibited tumour volume by 55% [1].
Reference:
Jones CD, Andrews DM, Barker AJ, et al. The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing. Bioorganic & Medicinal Chemistry Letters, 2008, 18(24): 6369-6373.
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