| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
NSC-622608 targets VISTA, an immune checkpoint protein that suppresses T-cell activation. VISTA is a negative regulator of the immune response, and its expression on tumor cells can allow them to evade immune attack. By binding to VISTA and blocking its function, NSC-622608 releases the brake on T-cell activation, promoting anti-tumor immunity. This mechanism is similar to that of other checkpoint inhibitors like PD-1 and CTLA-4 antibodies.
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| ln Vitro |
The VISTA-VSIG-3 interaction is disrupted by NSC622608, with an IC50 value of 9.7 ± 0.3 μM[1].
In vitro, NSC-622608 inhibits VISTA activity with an IC50 of 4.8 μM. It has been shown to attenuate the phosphorylation of the AKT/mTOR and JAK2/STAT5 pathways. In chronic myeloid leukemia (CML) cells, treatment with NSC-622608 resulted in reduced proliferation and induced apoptosis. These effects were observed in both imatinib-sensitive and imatinib-resistant CML cells. |
| ln Vivo |
In vivo, NSC-622608 has demonstrated antitumor activity in preclinical models. Studies have shown that its application significantly impeded CML cell proliferation and induced apoptosis. These findings support the potential of VISTA inhibition as a therapeutic strategy for cancer, particularly for tumors that are resistant to other therapies.
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| Enzyme Assay |
A cell-free assay for NSC-622608 would involve measuring its binding affinity to VISTA. In a FRET (Förster resonance energy transfer) assay, the compound has an IC50 of 4.8 μM. This type of assay confirms the compound's direct interaction with the VISTA protein. Specific protocols are not detailed in the available sources.
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| Cell Assay |
Cellular assays for NSC-622608 typically involve assessing its effects on immune cell function and cancer cell viability. The compound's ability to reverse VISTA-mediated suppression of T-cell activation can be measured in co-culture assays with T cells and VISTA-expressing cells. Its effects on cancer cell signaling and proliferation are assessed in various cancer cell lines.
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| Animal Protocol |
In vivo animal experiments with NSC-622608 have been conducted in models of CML. The compound's ability to inhibit tumor growth and induce apoptosis was demonstrated. Specific dosing regimens and detailed protocols are not provided in the available sources.
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| ADME/Pharmacokinetics |
NSC-622608 has a molecular formula and weight that are not specified in the sources, but it is a small molecule. Specific pharmacokinetic parameters are not provided. As a research compound, it is intended for preclinical studies. For storage, the powder should be kept at -20°C.
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| Toxicity/Toxicokinetics |
Toxicity data for NSC-622608 are not provided in the available sources. As a research compound targeting an immune checkpoint, it may have the potential for immune-related adverse events. It is intended for research use only and is not for human consumption.
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| References | |
| Additional Infomation |
NSC-622608 (CAS: 2593254-90-9) is a small-molecule ligand for VISTA. It is a novel inhibitor of this immune checkpoint with an IC50 of 4.8 μM. The compound is used in immuno-oncology research to study the role of VISTA in cancer immunity and to develop new therapeutic strategies. It is not an approved drug and is strictly for research purposes.
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| Molecular Formula |
C9H12BRN3OS2
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|---|---|
| Molecular Weight |
322.245078086853
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| Exact Mass |
320.96
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| CAS # |
2593254-90-9
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| PubChem CID |
360474
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
291
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Br.S1C(=N/C(=N/CC2=CC=CO2)/S1)N(C)C
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| InChi Key |
VVZWMEHUXGPOIY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H11N3OS2.BrH/c1-12(2)9-11-8(14-15-9)10-6-7-4-3-5-13-7;/h3-5H,6H2,1-2H3;1H
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| Chemical Name |
5-(furan-2-ylmethylimino)-N,N-dimethyl-1,2,4-dithiazol-3-amine;hydrobromide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~41.67 mg/mL (~129.31 mM)
H2O : ~12.5 mg/mL (~38.79 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 | 3.1032 mL | 15.5159 mL | 31.0318 mL | |
| 5 mM | 0.6206 mL | 3.1032 mL | 6.2064 mL | |
| 10 mM | 0.3103 mL | 1.5516 mL | 3.1032 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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