| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
(S)-BRD9500 is the inactive isomer and does not effectively inhibit PDE3 enzymes. BRD9500, the active compound, targets phosphodiesterase 3 (PDE3) enzymes, specifically PDE3A (IC50 = 10 nM) and PDE3B (IC50 = 27 nM). PDE3 inhibitors elevate intracellular cAMP levels, leading to downstream effects that include tumor cell killing.
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| ln Vitro |
(S)-BRD9500 exhibits minimal in vitro activity as a PDE3 inhibitor. In contrast, BRD9500 potently inhibits PDE3A with an IC50 of 10 nM and PDE3B with an IC50 of 27 nM, leading to increased cAMP levels, activation of downstream pathways, and SLFN12-dependent cancer cell death. (S)-BRD9500 is used as a control.
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| ln Vivo |
In vivo, (S)-BRD9500 is used as a control in animal models. BRD9500 demonstrates oral antitumor activity in xenograft models. (S)-BRD9500 should not produce the same level of efficacy, confirming that the therapeutic effect is mediated by the active isomer through PDE3 inhibition and the SLFN12-dependent pathway.
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| Enzyme Assay |
(S)-BRD9500 is used as a control in enzyme inhibition assays. For BRD9500, typical protocols involve incubating recombinant human PDE3A or PDE3B enzymes with varying concentrations of compound (0.1-1000 nM) in the presence of 0.1 uM cyclic nucleotide substrate (e.g., cAMP). Enzyme activity is measured by a fluorescence polarization or radioactive assay. (S)-BRD9500 is run in parallel.
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| Cell Assay |
Cell-based assays use (S)-BRD9500 as a control. Typical protocols involve treating cancer cells (e.g., SK-MEL-5 melanoma or HeLa cells) with BRD9500 or (S)-BRD9500 (0.01-10 uM) for 48-96 hours. Cell viability is assessed by CellTiter-Glo, and SLFN12 protein expression is verified by Western blot. (S)-BRD9500 should not induce cell death.
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| Animal Protocol |
In vivo, (S)-BRD9500 is used as a control in xenograft models. Typical protocols involve subcutaneous implantation of PDE3A/SLFN12-expressing cancer cells into immunocompromised mice. When tumors reach ~100-200 mm3, BRD9500 or (S)-BRD9500 (10-100 mg/kg, oral) is administered daily for 2-4 weeks, and tumor volume is monitored.
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| ADME/Pharmacokinetics |
No pharmacokinetic data specifically for (S)-BRD9500 is available. As a single enantiomer with the same molecular formula (C15H18FN3O2, MW 291.32) as BRD9500, it likely has similar PK properties but without the pharmacodynamic activity. BRD9500 is orally bioavailable with good in vivo exposure.
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| Toxicity/Toxicokinetics |
No direct toxicity data is available for (S)-BRD9500. As an inactive control compound, it is not expected to cause significant toxicity. BRD9500 has an acceptable safety profile in preclinical studies, but toxicity data for the (S)-enantiomer alone is not publicly available. Standard safety precautions apply.
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| 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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| Additional Infomation |
(S)-BRD9500 is a research-use compound and not a pharmaceutical for human consumption. BRD9500 is an orally active PDE3A/B inhibitor that induces SLFN12-dependent cancer cell killing and has been evaluated for antitumor activity in preclinical studies. (S)-BRD9500 is supplied for research use only. Neither BRD9500 nor (S)-BRD9500 has received regulatory approval.
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| CAS # |
1630760-76-7
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| Related CAS # |
BRD9500;1630760-75-6
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| Appearance |
Off-white to light yellow solid powder
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 200 mg/mL (686.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (17.16 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 50.0 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: ≥ 5 mg/mL (17.16 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 50.0 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: ≥ 5 mg/mL (17.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
Products are for research use only; We do not sell to patients
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