Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Targets |
PARP2 ( IC50 = 1 nM ); PARP1 ( IC50 = 2 nM ); TNKS1 ( IC50 = 50 nM ); TNKS2 ( IC50 = 50 nM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
In summary, cells are lysed for 20 minutes on ice in cell lysis buffer (CLB: 50 mM HEPES, pH 7.4, 150 mM NaCl, 1 mM MgCl2, 1 mM EGTA, 1 mM DTT, 1% TritonX-100, 1 μg/mL leupeptin, aprotinin, pepstatin, PMSF) after being washed three times in ice-cold PBS within 24 to 48 hours after transfection. Lysates undergo a 30-minute ultracentrifugation process at 100,000 g. After lysates are cleared, they are incubated with pre-bound protein A magnetic beads and anti-GFP antibody (3E6) for one hour at 4°C.
Following a 1-minute soak in CLB, beads are then washed for 3 minutes in CLB containing 1 M NaCl and 1 minute in PARP reaction buffer (PRB; 50 mM Tris, pH 7.5, 50 mM NaCl, 0.5 mM DTT, 0.1% TritonX-100, 1 μg/mL leupeptin, aprotinin, and pepstatin). For 30 minutes at 25°C, NAD+ incorporation reactions are carried out in PRB containing 10 μM NAD+ supplemented with 32P-NAD+ at a 1:20 ratio. NAD+ incorporation is carried out at a 1:5 ratio for one hour at 25°C for PARPs with low incorporation signals (PARP4, 5a, and 16). After that, the beads are once again suspended in Laemmli sample buffer, heated for ten minutes to 65°C, the beads are extracted with a magnet, and the supernatant is spotted onto Whatman paper. Phosphorimaging is used to analyze samples[1].
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Cell Assay |
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Animal Protocol |
Combination of Temozolomide (TMZ) and B16-F10 isograft model: B16-F10 cells (2 × 105) are subcutaneously injected into female C57BL/6 mice. One day after vaccination, medication treatment is started, with randomization based on body weight. Both TMZ and stenoparib are administered orally once daily and are both formulated in 0.5% methyl cellulose. Every day from day 1 to day 5, 50 mg/kg of TMZ is given either alone or in combination. Daily doses of 10, 30, and 100 mg/kg of tenoparib in combination with TMZ, as well as 100 mg/kg as a single agent, are given to patients on days 1 through 7. 0.5% methyl cellulose in water is the vehicle used to treat the control group. Animals receiving the combination are given TMZ after all animals have received their dose of stenoparib or the vehicle[1].
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References |
Molecular Formula |
C18H15N5O
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Molecular Weight |
317.34
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Exact Mass |
317.13
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Elemental Analysis |
C, 68.13; H, 4.76; N, 22.07; O, 5.04
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CAS # |
1140964-99-3
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
C1C2=CC=CC=C2CN1CC3=NC4=NNC(=O)C5=C4C(=CC=C5)N3
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InChi Key |
JLFSBHQQXIAQEC-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H15N5O/c24-18-13-6-3-7-14-16(13)17(21-22-18)20-15(19-14)10-23-8-11-4-1-2-5-12(11)9-23/h1-7H,8-10H2,(H,22,24)(H,19,20,21)
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Chemical Name |
11-(1,3-dihydroisoindol-2-ylmethyl)-2,3,10,12-tetrazatricyclo[7.3.1.05,13]trideca-1,5(13),6,8,11-pentaen-4-one
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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 | 3.1512 mL | 15.7560 mL | 31.5119 mL | |
5 mM | 0.6302 mL | 3.1512 mL | 6.3024 mL | |
10 mM | 0.3151 mL | 1.5756 mL | 3.1512 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.
Figure 1 E7449 traps PARP onto DNA and affects DNA repair pathways beyond HR.Oncotarget.2015 Dec 1;6(38):41307-23. th> |
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E7449 potentiates antitumor activity of temozolomide and carboplatin.Oncotarget.2015 Dec 1;6(38):41307-23. td> |
Antitumor activity and PARP inhibition by E7449 in a BRCA mutant xenograft model.Oncotarget.2015 Dec 1;6(38):41307-23. td> |
E7449 inhibits Wnt signalingin vitro: effects of E7449 treatment on Wnt proteins in SW480 cells by western blot analysis.Oncotarget.2015 Dec 1;6(38):41307-23. th> |
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E7449 inhibits Wnt signalingin vitro: effects of E7449 treatment on expression of Wnt-related genes in SW480 cells. Dose-dependent PARP inhibition by E7449 in tumor tissue from NCI-H460 human lung cancer xenografts. td> |
E7449 dose-responsively inhibits re-growth of hair, a Wnt-mediated pathway, in mice. Antitumor effect of E7449 in combination with MEK inhibitor in Wnt-dependent model.Oncotarget.2015 Dec 1;6(38):41307-23. td> |