| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
KM02894 targets glutamate release from cancer cells. Cancer cells release high levels of glutamate, which can disrupt normal bone turnover and may contribute to cancer-induced bone pain. By inhibiting glutamate release, KM02894 may help alleviate cancer-induced bone pain.
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| ln Vitro |
In vitro, KM02894 is an inhibitor of glutamate release. It has potential applications in cancer-related research, particularly in studying cancer-induced bone pain. Detailed IC50 values are not reported. It may modulate glutamatergic signaling in cancer cells.
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| ln Vivo |
In vivo, KM02894 can be used for cancer-related research, including studies on cancer-induced bone pain. By inhibiting glutamate release from cancer cells, it may help reduce bone pain and disruption of normal bone turnover. Animal studies are needed to confirm its in vivo efficacy and safety.
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| Enzyme Assay |
Cell-free assays for KM02894: glutamate release is measured using fluorometric or colorimetric glutamate assays. Cancer cells are treated with KM02894 at concentrations of 0.1-100 µM, and glutamate levels in the culture medium are measured. Inhibition percentages are calculated. Binding assays to potential targets can be performed using surface plasmon resonance or isothermal titration calorimetry.
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| Cell Assay |
Cellular assays for KM02894: cancer cell lines (e.g., breast cancer, prostate cancer) are cultured and treated with KM02894 at concentrations of 0.1-100 µM for 1-24 hours. Glutamate release is measured in the culture medium using fluorometric or colorimetric assays. Cell viability is assessed by MTT assay. Osteoclast activity is assessed in co-culture models to evaluate effects on bone turnover.
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| Animal Protocol |
In vivo animal studies for KM02894: animal models of cancer-induced bone pain would be used. Animals are implanted with cancer cells and treated with KM02894 orally or intraperitoneally at doses of 1-10 mg/kg. Bone pain is assessed by behavioral tests. Bone turnover markers and tumor growth are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of KM02894: as a small molecule (MW 215.30), it may have moderate oral bioavailability. It is soluble in DMSO (33.33 mg/mL, ~154.81 mM). Storage: powder at -20°C for up to 3 years; in solvent at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Toxicity of KM02894: comprehensive toxicity data are limited. As a glutamate release inhibitor, it may have effects on glutamatergic signaling in the nervous system. It is for research use only and not approved for clinical use.
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| References | |
| Additional Infomation |
KM02894 is a research compound with potential applications in cancer research, particularly in studying cancer-induced bone pain. It is a glutamate release inhibitor. No clinical trials or FDA approvals have been reported.
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| Molecular Formula |
C7H9N3OS2
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|---|---|
| Molecular Weight |
215.30
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| Exact Mass |
215.019
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| CAS # |
116850-74-9
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| PubChem CID |
2819872
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| Appearance |
White to off-white solid powder
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| LogP |
1.659
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
13
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| Complexity |
210
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNC(NNC(C1=CC=CS1)=O)=S
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| InChi Key |
SYXUJKFYUBHYNO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H9N3OS2/c1-8-7(12)10-9-6(11)5-3-2-4-13-5/h2-4H,1H3,(H,9,11)(H2,8,10,12)
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| Chemical Name |
1-methyl-3-(thiophene-2-carbonylamino)thiourea
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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: 33.33 mg/mL (154.81 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.61 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 25.0 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: ≥ 2.5 mg/mL (11.61 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 25.0 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: ≥ 2.5 mg/mL (11.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6447 mL | 23.2234 mL | 46.4468 mL | |
| 5 mM | 0.9289 mL | 4.6447 mL | 9.2894 mL | |
| 10 mM | 0.4645 mL | 2.3223 mL | 4.6447 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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