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Ulevostinag (MK-1454; MK1454) is an investigational small molecule STING agonist with potential immunomodulatory and anticancer activities. It can be administered as an intratumoral injection and is currently being evaluated in a Phase 1 clinical trial for the treatment of solid tumors and lymphomas (ClinicalTrials.gov, NCT03010176). STING is a signaling molecule that plays an important role in the body’s first line of defense against pathogens, such as bacteria and viruses (innate immune system). When activated, STING triggers the production of inflammatory proteins that can stimulate the immune system leading to the deployment of T cells, which are important in generating an effective immune mediated response to cancer cells. MK-1454 exhibited robust tumor cytokine upregulation and effective antitumor activity. Tumor shrinkage in mouse models that are intrinsically resistant to single-agent therapy was further enhanced when treating the animals with MK-1454 in combination with a fully murinized antimouse PD-1 antibody, mDX400.
| ln Vivo |
MK-1454, also known as ulevostinag, has the ability to stimulate the immune system against tumors injected with MC38 (5 μg, 20 μg, intratumoral injection) and suppress the growth of untouched tumors [1]. MC38 and B16F10 tumor regression mice models showed complete tumor regression when urevostinag (MK-1454) (4) μg, intratumoral injection on days 0, 3, and 7) was administered. This also improved the outcome of anti-PD1 treatment [1].
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| Animal Protocol |
Animal/Disease Models: MC38 colon adenocarcinoma tumor-bearing mice [1]
Doses: 5 μg, 20 μg Route of Administration: Intratumoral Experimental Results: Injected (right) tumor regression and regression of injected and uninjected tumors at dose 20 μg and detected in plasma. IFN-β and the proinflammatory cytokines IL-6 and TNF-α were elevated in injected tumors. Animal/Disease Models: MC38 and B16F10 tumor mouse models [1] Doses: 4 μg Route of Administration: intratumoral Experimental Results: Improved tumor growth inhibition, complete remission in 7 out of 10 mice within 28 days. |
| References |
| Molecular Formula |
C20H22F2N10O9P2S2
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| Molecular Weight |
710.52
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| CAS # |
2082743-96-0
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| Related CAS # |
Ulevostinag (isomer 1);2231258-61-8
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| Appearance |
White to off-white solid powder
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| SMILES |
O=C1NC(N)=NC2N([C@H]3[C@]4(C([C@@]([H])(CO[P@@](=O)(S)O[C@@]5([C@]([H])(O[C@H]([C@H]5F)N5C=NC6C(N)=NC=NC5=6)CO[P@@](S)(O4)=O)[H])O3)(F)[H])[H])C=NC1=2
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| Chemical Name |
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| Synonyms |
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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 |
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| 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) |
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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 | 1.4074 mL | 7.0371 mL | 14.0742 mL | |
| 5 mM | 0.2815 mL | 1.4074 mL | 2.8148 mL | |
| 10 mM | 0.1407 mL | 0.7037 mL | 1.4074 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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