| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
Cyclin E-cdk2, Cyclin A-cdk2, Cyclin B1-cdk1, p25-cdk5, Cyclin D3-cdk6, and Cyclin T-cdk9 are all efficiently inhibited by AZD5438. activity (16, 21, 20 nM, 6, 45 nM). Cyclin E-cdk2, Cyclin A-cdk2, Cyclin B1-cdk1, p25-cdk5, Cyclin D3-cdk6, and Cyclin T-cdk9 are all potently inhibited by AZD5438. Similar to numerous other CDK regulators, AZD5438 suppresses p25-cdk5 and glycogen synthase, which in turn control the sporadic activity of 3β (IC50 values of 14 and 17 nM, correspondingly) [1]. The cellular radiation targeting of NSCLC cells is greatly improved by AZD5438. AZD5438 can also improve tumor growth delay when used in conjunction with radiation therapy, with an improved cell range of 1.2–1.7 [2].
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| ln Vivo |
AZD5438 (50 mg/kg twice day or 75 mg/kg for oncology) prevents human xenografts from growing. AZD5438 lowers the percentage of circulating active cells internally. Additional pharmacodynamic investigation of SW620 xenografts treated with AZD5438 revealed that after a single threshold of 16 hours, effective dosages of AZD5438 (>40% tumor growth suppression) maintained inhibitory effects on biomarkers including phospho-pRbSer249/Thr252[1].
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| References |
[1]. Byth KF, et al. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol Cancer Ther. 2009 Jul;8(7):1856-66. Epub 2009 Jun 9.
[2]. Raghavan P, et al. AZD5438, an Inhibitor of Cdk1, 2, and 9, Enhances the Radiosensitivity of Non-Small Cell Lung Carcinoma Cells. Int J Radiat Oncol Biol Phys. 2012 Jul 12 |
| Molecular Formula |
C18H21N5O2S
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|---|---|
| Molecular Weight |
371.46
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| CAS # |
602306-29-6
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| SMILES |
CC1=NC=C(N1C(C)C)C2=NC(=NC=C2)NC3=CC=C(C=C3)S(=O)(=O)C
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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) |
DMSO : ~100 mg/mL (~269.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 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 (6.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6921 mL | 13.4604 mL | 26.9208 mL | |
| 5 mM | 0.5384 mL | 2.6921 mL | 5.3842 mL | |
| 10 mM | 0.2692 mL | 1.3460 mL | 2.6921 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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