| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
KIAA1363 (also known as AADACL1), a 2-acetyl monoacylglycerol ether (MAGE) hydrolase. This enzyme is upregulated in invasive cancer cells of various tissues, such as ovarian, breast, and prostate cancers, where it is involved in lipid metabolism and signaling pathways that contribute to tumor aggressiveness. AS115 is a selective inactivator of KIAA1363, inhibiting its hydrolase activity.
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| ln Vitro |
AS115 (10 μM, 4 h) significantly reduced the formation of MAGE, alkyllysophosphatidylcholine, and alkyllysophosphatidic acid in SKOV3 cells [1].
AS115 inhibits KIAA1363 with an IC50 of 150 nM in the invasive ovarian cancer cell line SKOV3. This demonstrates the compound's potent activity against the target enzyme in a complex cellular environment relevant to cancer biology. The compound is a selective inactivator, meaning it likely binds covalently to the enzyme, leading to sustained target inhibition. |
| ln Vivo |
No specific in vivo data for AS115 was found. As a selective inactivator of the cancer-associated enzyme KIAA1363, AS115 is expected to have a biological impact in vivo. Since KIAA1363 is not highly expressed in most normal tissues but is upregulated in aggressive cancers, an inhibitor could potentially suppress tumor growth or invasiveness without significant toxicity.
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| Enzyme Assay |
Standard KIAA1363 hydrolase activity assay: The assay uses a fluorogenic substrate, such as 4-methylumbelliferyl (4-MU) acetate or a MAGE analog. Recombinant KIAA1363 protein or cell lysates (from SKOV3 cells) are incubated in a reaction buffer with the substrate. AS115 is added at a range of concentrations and pre-incubated with the enzyme. After a set time, the fluorescence of the released 4-MU is measured (Ex 360 nm/Em 460 nm) to calculate the IC50.
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| Cell Assay |
Standard cell viability and target engagement assay: SKOV3 ovarian cancer cells are seeded in 96-well plates and treated with increasing concentrations of AS115 for 24-72 hours. Cell viability is measured using an MTT or CellTiter-Glo assay. To confirm target engagement, cells are treated with AS115, and the cell lysates are used in an in vitro hydrolase activity assay as described above. Inhibition of cellular hydrolase activity by AS115 is measured.
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| Animal Protocol |
No specific animal protocol was found. To test the efficacy of AS115 in an ovarian cancer model, female BALB/c nude mice would be injected intraperitoneally or subcutaneously with SKOV3 cells to establish tumors. Once tumors reach a predetermined size, mice would be treated with AS115 (e.g., 10-50 mg/kg) via intraperitoneal (IP) injection daily. Tumor volume, body weight, and survival rates would be monitored to assess efficacy and toxicity.
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| ADME/Pharmacokinetics |
No specific PK data was found. As a small-molecule enzyme inactivator, AS115 is expected to have a PK profile suitable for in vivo research. It is likely to be metabolized by the liver and may have a long duration of action due to its inactivation mechanism. Standard PK studies in rodents are required to determine its half-life, clearance, and bioavailability.
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| Toxicity/Toxicokinetics |
No specific toxicity data was found. As a selective inactivator of KIAA1363, which is not essential in normal tissues, AS115 is expected to have a favorable safety profile. However, extensive toxicity testing in animal models is necessary to evaluate potential off-target effects before it can be considered a clinical candidate.
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| References |
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| Additional Infomation |
AS115 (CAS: 926657-43-4) has a molecular formula of C21H32FNO4 and a molecular weight of 381.5. It is a potent and selective inactivator of KIAA1363 (IC50 = 150 nM). This compound is used for research into the role of lipid metabolism in aggressive cancers.
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| Molecular Formula |
C21H32FNO4
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|---|---|
| Molecular Weight |
381.48
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| CAS # |
926657-43-4
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| Appearance |
Typically exists as solids at room temperature
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
460.3±43.0 °C at 760 mmHg
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| Flash Point |
232.2±28.2 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.491
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| LogP |
4.74
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| SMILES |
CCCCOC[C@@H]1CCCC[C@@H]1COCCNC(OC2=CC=CC=C2F)=O
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.6214 mL | 13.1068 mL | 26.2137 mL | |
| 5 mM | 0.5243 mL | 2.6214 mL | 5.2427 mL | |
| 10 mM | 0.2621 mL | 1.3107 mL | 2.6214 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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