| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Aurora A 45 nM (IC50)
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|---|---|
| ln Vitro |
In MYCN-amplified neuroblastoma cell lines SK-N-BE(2) and Kelly, CD532 (1-10000 nM; 72 h) is cytotoxic, with EC50s of 223.2 nM and 146.7 nM, respectively[1]. MYCN protein in SK-N-BE(2) cells is lost in a dose-dependent manner upon exposure to CD532 (0.1–1 μM; 24 h)[1]. SK-N-BE(2) cells are prevented from entering S-phase by CD532 (1 μM; 6 h)[1].
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| ln Vivo |
In mice with subcutaneous sonic hedgehog (SHH)-subtype medulloblastoma, CD532 (25 mg/kg; ip twice weekly for 3 weeks) reduces the tumor volume and improves survival[1]. MYCN-amplified neuroblastoma xenografts produce less MYCN protein when treated with CD532 (60 mg/kg; intraperitoneally for two days)[1]. In mice, CD532 (20 mg/kg; ip) exhibits an AUC0-24 of 27 μM·h and a serum half-life of approximately 1.5 hours[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SK-N-BE(2) and Kelly cells Tested Concentrations: 1, 10, 100, 1000, 10000 nM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the cell viability of SK-N-BE(2) and Kelly cells, with EC50s of 223.2 nM and 146.7 nM, respectively. Cell Cycle Analysis[1] Cell Types: SK-N-BE(2) cells Tested Concentrations: 1 μM Incubation Duration: 4 hrs (hours) Experimental Results: Resulted in a rapid and potent loss of S-phase and accumulation in both G0/G1 and G2. Western Blot Analysis[1] Cell Types: SK-N-BE(2) cells Tested Concentrations: 0.1, 0.25, 0.5, 1 μM Incubation Duration: 2, 4, 6, 24 hrs (hours) Experimental Results: Causes dose-dependent and time-dependent loss of MYCN protein. |
| Animal Protocol |
Animal/Disease Models: Homozygous nu/nu (nude) mice with SHH-subtype MYCN-expressing medulloblastoma[1]
Doses: 25 mg/kg Route of Administration: Ip twice weekly for 3 weeks Experimental Results: diminished the level of MYCN protein and tumor volume and increases survival. |
| References |
[1]. Gustafson WC, et, al. Drugging MYCN through an allosteric transition in Aurora kinase A. Cancer Cell. 2014 Sep 8;26(3):414-427.
[2]. Lee JK, et, al. N-Myc Drives Neuroendocrine Prostate Cancer Initiated from Human Prostate Epithelial Cells. Cancer Cell. 2016 Apr 11;29(4):536-547. |
| Molecular Formula |
C26H25F3N8O
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|---|---|
| Molecular Weight |
522.52
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| CAS # |
1639009-81-6
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| Related CAS # |
CD532 hydrochloride;2926498-81-7
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| SMILES |
FC(C1C=CC=C(C=1)NC(NC1C=CC(=CC=1)NC1=NC=CC(=N1)NC1C=C(C2CCCC2)NN=1)=O)(F)F
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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 : 250 mg/mL (478.45 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.98 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 20.8 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: ≥ 2.08 mg/mL (3.98 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 20.8 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: ≥ 2.08 mg/mL (3.98 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 | 1.9138 mL | 9.5690 mL | 19.1380 mL | |
| 5 mM | 0.3828 mL | 1.9138 mL | 3.8276 mL | |
| 10 mM | 0.1914 mL | 0.9569 mL | 1.9138 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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