| Size | Price | Stock | Qty |
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| Targets |
DGKζ[1]
Diacylglycerol kinase zeta (DGKζ). BAY 2965501 is a potent and specific inhibitor of DGKζ. DGKζ is a lipid kinase that phosphorylates diacylglycerol (DAG) to phosphatidic acid (PA), thereby regulating DAG-mediated signaling pathways. DGKζ is overexpressed in certain cancer cells and plays an important role in tumor cell survival and immunosuppression. |
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| ln Vitro |
BAY 2965501 improves the activation of natural killer cells induced by IL-2 and the destruction of tumor cells by T cells and natural killer cells [2].
BAY 2965501 is a potent and specific DGKζ inhibitor. It induces pERK activation. In vitro, BAY 2965501 improves the activation of natural killer cells induced by IL-2 and enhances the destruction of tumor cells by T cells and natural killer cells. It modulates DAG-regulated cellular signaling pathways. |
| ln Vivo |
In the F9 testicular teratoma model, BAY-2965501 suppresses tumor growth. Additionally, immune checkpoint blockade and BAY-2965501 together may have additive or synergistic effects [3].
In vivo, BAY 2965501 suppresses tumor growth in the F9 testicular teratoma model. Additionally, immune checkpoint blockade and BAY 2965501 together may have additive or synergistic effects. The compound is being investigated for cancer immunotherapy. It is in Phase I clinical development. |
| Enzyme Assay |
In vitro enzyme activity assays for BAY 2965501 involve measuring its ability to inhibit DGKζ kinase activity. Recombinant DGKζ enzyme is incubated with its substrate (diacylglycerol) in the presence of ATP and increasing concentrations of the compound. Kinase activity is measured by detecting the production of phosphatidic acid or by using radiolabeled ATP incorporation assays.
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| Cell Assay |
In vitro cellular assays for BAY 2965501 involve treating immune cells (such as T cells and NK cells) with the compound and measuring its effects on cell activation and tumor cell killing. Readouts include pERK activation, cytokine production, and cytotoxicity assays.
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| Animal Protocol |
In vivo efficacy of BAY 2965501 is evaluated in animal models of cancer, such as the F9 testicular teratoma model. The compound is administered orally. Efficacy endpoints include tumor growth suppression and survival. Combination studies with immune checkpoint inhibitors are also being explored.
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| ADME/Pharmacokinetics |
BAY 2965501 has a molecular weight of 414.45 g/mol and a molecular formula of C20H19FN4O3S. It has an XLogP3-AA of 4.3, indicating moderate lipophilicity. The compound is orally bioavailable and soluble in DMSO (≥100 mg/mL). Powder stability is 3 years at -20°C.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for BAY 2965501 in the provided literature. As a therapeutic candidate for cancer immunotherapy, its safety profile is being evaluated in Phase I clinical trials. Potential toxicities could be related to its immunomodulatory effects.
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| References |
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| Additional Infomation |
Veludacigib is an orally bioavailable diacylglycerol kinase ζ (DGKζ) inhibitor with potential antitumor activity. Oral administration of veludacigib inhibits DGKζ activity, thereby preventing the phosphorylation of diacylglycerol (DAG) to phosphatidic acid (PA) and modulating DAGζ-regulated cellular signaling pathways. This may inhibit the proliferation of tumor cells with overactivated DGKζ. DGKζ is overexpressed in some cancer cells and plays an important role in tumor cell survival. DAGζ may also play a crucial role in tumor immunosuppression.
BAY 2965501 (Veludacigib) is an orally bioavailable, potent, and specific inhibitor of DGKζ. It induces pERK activation and enhances immune cell-mediated tumor cell destruction. BAY 2965501 suppresses tumor growth in preclinical models and is in Phase I clinical development for cancer immunotherapy. It has a molecular formula of C20H19FN4O3S and a molecular weight of 414.45. |
| Molecular Formula |
C20H19FN4O3S
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|---|---|
| Molecular Weight |
414.45
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| Exact Mass |
414.116
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| CAS # |
2732902-08-6
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| Related CAS # |
(S)-BAY 2965501;2732902-09-7
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| PubChem CID |
166792554
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
582
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1C=C(C=CC=1OC)C(C1SC(N([C@@H](C(N)=O)C)C2C=CC(=CC=2)F)=NC=1N)=O
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| InChi Key |
HSBUVKDEUUJREZ-LLVKDONJSA-N
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| InChi Code |
InChI=1S/C20H19FN4O3S/c1-11(19(23)27)25(14-7-5-13(21)6-8-14)20-24-18(22)17(29-20)16(26)12-3-9-15(28-2)10-4-12/h3-11H,22H2,1-2H3,(H2,23,27)/t11-/m1/s1
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| Chemical Name |
(2R)-2-(N-[4-amino-5-(4-methoxybenzoyl)-1,3-thiazol-2-yl]-4-fluoroanilino)propanamide
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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: ≥ 100 mg/mL (241.28 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 | 2.4128 mL | 12.0642 mL | 24.1284 mL | |
| 5 mM | 0.4826 mL | 2.4128 mL | 4.8257 mL | |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4128 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05614102
Conditions:Advanced Solid TumorsProducts are for research use only; We do not sell to patients
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