| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
BAY 2666605 targets phosphodiesterase 3A (PDE3A) and phosphodiesterase 3B (PDE3B). It acts as an inhibitor and also induces the formation of the PDE3A-SLFN12 complex. By inhibiting PDE3A and inducing the PDE3A-SLFN12 complex, BAY 2666605 exerts anti-cancer effects across multiple cancer types.
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| ln Vitro |
Brain cancer (especially glioma, more specifically glioblastoma and astrocytoma), breast cancer (especially ductal carcinoma and adenocarcinoma), cervical cancer, AML (especially erythroleukemia), lung cancer (especially NSCLC adenocarcinoma) and SCLC, skin cancer (especially melanoma), esophageal cancer (especially squamous cell carcinoma), ovarian cancer (especially teratoma fetal cancer, adenocarcinoma), pancreatic cancer, and prostate cancer are all effectively inhibited by BAY 2666605 (Example 135) [1].
In vitro, BAY 2666605 inhibits PDE3A and PDE3B with IC50 values of 87 nM and 50 nM, respectively. It shows anti-proliferative activity against a broad range of cancer cell lines, including those from brain, breast, lung, skin, esophageal, ovarian, pancreatic, and prostate cancers. |
| ln Vivo |
In a mouse xenograft model of human cancer, treatment with BAY 2666605 (5 mg/kg; oral; twice daily) showed antitumor effectiveness [1].
In vivo activity data for BAY 2666605 are not extensively detailed in the available sources. The compound is orally active and is being investigated in clinical trials for its potential as a targeted anticancer agent. Specific in vivo efficacy data are not provided. |
| Enzyme Assay |
The in vitro enzyme assay for BAY 2666605 involves measuring the inhibition of PDE3A and PDE3B activity. Recombinant enzymes are incubated with a substrate (e.g., cAMP) in the presence of varying compound concentrations. The IC50 values are determined by quantifying the reduction in substrate hydrolysis using techniques such as radioactive or fluorescence-based assays.
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| Cell Assay |
Cellular assays are performed using cancer cell lines. Cells are treated with BAY 2666605 at various concentrations, and cell viability is assessed using assays such as MTT or CellTiter-Glo. The induction of the PDE3A-SLFN12 complex is confirmed by co-immunoprecipitation or proximity ligation assays.
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| Animal Protocol |
In vivo animal studies for BAY 2666605 are not detailed in the available sources. The compound is being investigated in clinical trials for its potential as a targeted anticancer agent. Specific animal models and dosing regimens are not described.
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| ADME/Pharmacokinetics |
BAY 2666605 is an orally active compound. It is being investigated in clinical trials, indicating favorable pharmacokinetic properties. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
Toxicity data for BAY 2666605 are not reported in the available sources. As an investigational compound in clinical trials, it has been evaluated for safety, but specific toxicological profiles are not available.
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| References | |
| Additional Infomation |
SLFN12-PDE3A complex inducer BAY 2666605 is an orally bioavailable drug that induces the formation of a complex between Schlafen family member 12 (SLFN12) and phosphodiesterase 3A (PDE3A), exhibiting potential antitumor activity. After oral administration, BAY 2666605 induces the formation of the SLFN12-PDE3A complex. This complex stabilizes SLFN12 and alters the expression of a group of genes regulating cell survival, death, and proliferation. This inhibits cell cycle progression and induces apoptosis in cancer cells that specifically overexpress both proteins.
BAY 2666605 is an investigational anticancer agent in clinical trials. It is a PDE3A-SLFN12 complex inducer with a novel mechanism of action. The compound shows broad anti-cancer activity across multiple cancer types. It is available for research purposes. |
| Molecular Formula |
C17H12F4N2O2
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|---|---|
| Molecular Weight |
352.28
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| Exact Mass |
352.083
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| CAS # |
2275774-60-0
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| PubChem CID |
137465182
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| Appearance |
White to off-white solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
529
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O1[C@@H](C)C(C2=CC=C(C3=CC=C(F)C=C3)C(C(F)(F)F)=C2)=NNC1=O
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| InChi Key |
JNTJTCXFIXNXDV-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C17H12F4N2O2/c1-9-15(22-23-16(24)25-9)11-4-7-13(14(8-11)17(19,20)21)10-2-5-12(18)6-3-10/h2-9H,1H3,(H,23,24)/t9-/m0/s1
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| Chemical Name |
(6S)-5-[4-(4-fluorophenyl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-1,3,4-oxadiazin-2-one
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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) |
DMSO : ~250 mg/mL (~709.66 mM)
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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 | 2.8387 mL | 14.1933 mL | 28.3865 mL | |
| 5 mM | 0.5677 mL | 2.8387 mL | 5.6773 mL | |
| 10 mM | 0.2839 mL | 1.4193 mL | 2.8387 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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