| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
AZD-5597 targets CDK1 and CDK2, key regulators of the cell cycle. It is a potent imidazole pyrimidine amide CDK inhibitor. By inhibiting CDK1 and CDK2, it disrupts cell cycle progression and inhibits the proliferation of tumor cells. The compound has excellent physiochemical properties and large margins against inhibition of CYP isoforms and the hERG ion channel.
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|---|---|
| ln Vitro |
In vitro, AZD-5597 inhibits CDK1 and CDK2 with IC50 values of 2 nM each. It exhibits significant antiproliferative activity against human LoVo cells with an IC50 of 39.0 nM. It has potent anti-proliferative effects against a range of cancer cell lines. Its high specificity and bioactivity make it ideal for exploring targeted cancer therapies.
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| ln Vivo |
Specific in vivo data for AZD-5597 are not detailed in the available literature. However, as a potent CDK inhibitor with anti-tumor activity, it could be used in preclinical studies to investigate cell cycle control, apoptosis induction, and combination therapy strategies. Its excellent physiochemical properties suggest it may have favorable pharmacokinetics.
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| Enzyme Assay |
The enzymatic activity of AZD-5597 can be assessed using kinase assays with recombinant CDK1 and CDK2. The kinases are incubated with their substrates (e.g., histone H1) and ATP in the presence of varying concentrations of the inhibitor. The extent of phosphorylation is measured using techniques such as radioactive labeling or immunoassay. The IC50 values for CDK inhibition are determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of AZD-5597, cancer cells such as LoVo are treated with the compound. Cell proliferation and viability are assessed using standard assays such as MTT or CellTiter-Glo. Cell cycle progression is analyzed by flow cytometry. The effects on CDK activity and downstream signaling pathways are assessed by Western blotting.
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| Animal Protocol |
In vivo studies with AZD-5597 would typically involve administration to tumor-bearing mice in xenograft models. The compound's effects on tumor growth, cell cycle markers, and apoptosis would be assessed. Pharmacokinetic parameters and toxicity would also be evaluated.
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| ADME/Pharmacokinetics |
AZD-5597 has a molecular formula of C23H28FN7O and a molecular weight of 437.51. Its CAS number is 924641-59-8. The compound is a potent imidazole pyrimidine amide CDK inhibitor. It is soluble in DMSO and other organic solvents. The purity is typically >97%.
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| Toxicity/Toxicokinetics |
Specific toxicology data for AZD-5597 are not detailed in the available literature. However, its large margins against inhibition of CYP isoforms and the hERG ion channel suggest a potentially favorable safety profile. As with all research compounds, standard safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
AZD-5597 is a potent CDK1/2 inhibitor used in cancer research. It has potent anti-proliferative effects against a range of cancer cell lines. It is a valuable tool for studying cell cycle regulation and for developing targeted cancer therapies. It is not a clinically approved drug.
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| Molecular Weight |
437.5131
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|---|---|
| Exact Mass |
437.234
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| CAS # |
924641-59-8
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| PubChem CID |
16113484
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.947
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
630
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=NC=C(N1C(C)C)C2=NC(=NC=C2F)NC3=CC=C(C=C3)C(=O)N4CC[C@@H](C4)NC
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| InChi Key |
NTSDIJMNXYJJNG-SFHVURJKSA-N
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| InChi Code |
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
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| 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
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2857 mL | 11.4283 mL | 22.8566 mL | |
| 5 mM | 0.4571 mL | 2.2857 mL | 4.5713 mL | |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2857 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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