| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
ARTD1/PARP1 ( IC50 = 4.4 μM ); ARTD10/PARP10 ( IC50 = 0.8 μM ); ARTD8/PARP14 ( IC50 = 1.6 μM ); ARTD7/PARP15 ( IC50 = 1.7 μM )
ARTD10/PARP10-IN-1 targets multiple members of the PARP family, including ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10, and ARTD1/PARP1. These enzymes are involved in the post-translational modification of proteins by adding either single (MARylation) or multiple (PARylation) ADP-ribose units. This modification plays a crucial role in various cellular processes, including DNA repair, transcription, and cell signaling. By inhibiting these enzymes, the compound disrupts these pathways, which is particularly relevant in the context of cancer, where DNA repair pathways are often dysregulated. |
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| ln Vitro |
In vitro, ARTD10/PARP10-IN-1 demonstrates potent inhibitory activity against its targets. It has an IC50 of 0.8 μM for ARTD10/PARP10, 1.6 μM for ARTD8/PARP14, 1.7 μM for ARTD7/PARP15, and 4.4 μM for ARTD1/PARP1. This broad-spectrum activity makes it a useful tool for studying the collective effects of PARP family inhibition, although its lack of selectivity limits its use for dissecting the function of a single enzyme. Its potential for anticancer and antitumor activity is being investigated, particularly for prostate and breast cancers.
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| ln Vivo |
In vivo data for ARTD10/PARP10-IN-1 is limited, as it is primarily used as a chemical probe for in vitro and mechanistic studies. However, its ability to inhibit multiple PARP family members suggests it could have antitumor activity in xenograft models of cancers with DNA repair deficiencies. Specific animal studies, including dosing regimens and administration routes, are not detailed in the available literature. Its primary application is in cellular models to investigate the effects of PARP inhibition.
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| Enzyme Assay |
The inhibitory activity of ARTD10/PARP10-IN-1 is assessed using cell-free enzymatic assays. Recombinant enzymes (PARP1, PARP10, PARP14, PARP15) are incubated with their respective substrates (e.g., NAD⁺) and varying concentrations of the test compound. The level of ADP-ribosylation is then measured, typically using a TR-FRET or chemiluminescent-based detection method. The IC50 values are calculated from the resulting dose-response curves.
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| Cell Assay |
The cellular activity of ARTD10/PARP10-IN-1 is evaluated in various cancer cell lines, such as those from prostate and breast cancers. Cells are treated with serial dilutions of the compound, and its effect on cell viability and proliferation is assessed using standard assays like MTT or CellTiter-Glo. The compound's ability to induce apoptosis or cell cycle arrest is also investigated. The effect on PARP activity in cells can be confirmed by Western blot using antibodies specific for PAR or MAR.
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| Animal Protocol |
In vivo studies for ARTD10/PARP10-IN-1 would typically involve administering the compound to immunodeficient mice bearing subcutaneous xenografts of human cancer cell lines. Mice would be randomized to receive vehicle or the compound at various doses via oral gavage or intraperitoneal injection. Tumor volume would be measured, and at study termination, tumors would be harvested for pharmacodynamic analysis, including assessment of PARP activity and apoptosis markers.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of ARTD10/PARP10-IN-1 are not extensively documented in the available literature. As a small molecule (MW 248.23), it may have moderate oral bioavailability. Its solubility in DMSO is expected to be adequate for in vitro studies. For any in vivo use, researchers would need to determine its solubility in suitable vehicles and perform pilot PK studies to establish appropriate dosing regimens. The compound should be stored at low temperatures.
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| Toxicity/Toxicokinetics |
Toxicology data for ARTD10/PARP10-IN-1 is not publicly available, as it is a research compound and not intended for human therapeutic use. Its safety profile has not been established in formal toxicology studies. As a broad-spectrum PARP inhibitor, it may have a higher potential for off-target effects compared to more selective compounds. The compound is for research use only and should not be used in humans.
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| References | |
| Additional Infomation |
ARTD10/PARP10-IN-1 (CAS: 1708103-76-7) is a potent, multi-target PARP inhibitor used as a research tool. With a molecular weight of 248.23 and a chemical formula of C12H12N2O4, it is a valuable compound for studying the role of PARP family members in cancer biology. Its inhibition of both mono- and poly-ADP-ribosyltransferases makes it a useful tool for exploring the combined effects of blocking multiple ADP-ribosylation pathways.
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| Molecular Formula |
C12H12N2O4
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|---|---|
| Exact Mass |
248.08
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| CAS # |
1708103-76-7
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| PubChem CID |
118732826
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
0.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
365
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC(=O)/C=C\C(=O)NC1=CC=CC(=C1)C(=O)N
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| InChi Key |
KXULAXICDCSUDZ-WAYWQWQTSA-N
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| InChi Code |
InChI=1S/C12H12N2O4/c1-18-11(16)6-5-10(15)14-9-4-2-3-8(7-9)12(13)17/h2-7H,1H3,(H2,13,17)(H,14,15)/b6-5-
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| Chemical Name |
methyl (Z)-4-(3-carbamoylanilino)-4-oxobut-2-enoate
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| Synonyms |
ARTD10/PARP10-IN-1
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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.) |
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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