| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
PDE3A 10 nM (IC50) PDE3B 27 nM (IC50)
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|---|---|
| ln Vitro |
An analog for DNMDP is BRD9500. By causing PDE3A/B interactions with SFLN12, DNMDP potently and specifically inhibits PDE3A and PDE3B, hence killing cancer cells[1]. In terms of SK-MEL-3 melanoma cell line viability, BRD9500 has an EC50 of 1 nM[1]. BRD9500 has a 1.6 nM EC50 for HeLa viability [1]. In HeLa cells, the PDE3A-SLFN12 interaction is stabilized by BRD9500 (10 μM; 8 hours)[1].
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| ln Vivo |
In mice, BRD9500 (10, 20, and 50 mg/kg; orally) suppresses the growth of SK-MEL-3 melanoma[1]. BRD9500 is a good option for in vivo xenograft testing since it exhibits high plasma levels in mice following intravenous (1 mg/kg) and oral (2 mg/kg) administration over an eight-hour period[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: HeLa cells Tested Concentrations: 10 μM Incubation Duration: 8 hrs (hours) Experimental Results: SLFN12 coimmunoprecipitation was analyzed by immunoblotting with an anti-V5 antibody to detect the SLFN12-V5 fusion protein. The SLFN12-V5 was clearly detected with the anti-V5 antibody. |
| Animal Protocol |
Animal/Disease Models: Female NMRI nude mice bearing SK-MEL-3 melanoma cells tumor xenografts[1]
Doses: 10, 20, and 50 mg /kg Route of Administration: Orally at 10 and 20 mg/kg twice (two times) daily (2QD) and at 50 mg/kg once per day (QD). Experimental Results: Achieved the strongest antitumor activity at 50 mg/kg. All treatments were well tolerated without critical body weight loss or toxicities. |
| References |
[1]. Timothy A Lewis, et al. Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing. ACS Med Chem Lett. 2019 Oct 18;10(11):1537-1542.
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| Molecular Formula |
C15H18FN3O2
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|---|---|
| Molecular Weight |
291.32
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| CAS # |
1630760-75-6
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| Related CAS # |
(S)-BRD9500;1630760-76-7
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| SMILES |
FC1C=C(C=CC=1N1CCOCC1)C1[C@H](C)CC(NN=1)=O
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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: 50 mg/mL (171.63 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.58 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 (8.58 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 (8.58 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 | 3.4327 mL | 17.1633 mL | 34.3265 mL | |
| 5 mM | 0.6865 mL | 3.4327 mL | 6.8653 mL | |
| 10 mM | 0.3433 mL | 1.7163 mL | 3.4327 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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