AZD-5597 |
Catalog No.GC12826
One-Click Copy Product Info
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Potent CDK inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 924641-59-8
Sample solution is provided at 25 µL, 10mM.
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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:
[1].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.
| Cas No. | 924641-59-8 | SDF | |
| Chemical Name | (S)-(4-((5-fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl)amino)phenyl)(3-(methylamino)pyrrolidin-1-yl)methanone | ||
| Canonical SMILES | CC(N1C(C)=NC=C1C2=NC(NC3=CC=C(C(N4CC[C@@](NC)([H])C4)=O)C=C3)=NC=C2F)C | ||
| Formula | C23H28FN7O | M.Wt | 437.51 |
| Solubility | ≥ 15.65mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2857 mL | 11.4283 mL | 22.8566 mL |
| 5 mM | 457.1 μL | 2.2857 mL | 4.5713 mL |
| 10 mM | 228.6 μL | 1.1428 mL | 2.2857 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)