| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PARP1-IN-44 (Compound B3) (3.63-100 μM, 5 days) exhibits anti-proliferative activity against various tumor cells, with IC50 values of 9.70 μM (HCT-15), 5.80 μM (HCC1937), 18.06 μM (HepG2), 16.48 μM (MCF7), 9.88 μM (Capan-1), and 12.48 μM (CT26), respectively. It also shows excellent safety, with IC50 values greater than 100 μM against non-cancerous NCM460 and GES-1 cell lines [1]. PARP1-IN-44 (2.5-10 μM, 48 hours) can induce apoptosis in HCC1937 cells and cause cell cycle arrest [1]. PARP1-IN-44 (2.5-10 μM, 24 h) can inhibit PARP1-mediated H2O2-induced DNA damage repair in HCC1937 cells[1]. PARP1-IN-44 (2.5-10 μM, 24 h) can induce ROS accumulation (detected by DCFH-DA probe) and mitochondrial depolarization (assessed by JC-1 staining) in HCC1937 cells[1]. PARP1-IN-44 (0.25-2 μM, 72 h) can restore the innate immune response in CT26 cells[1].
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|---|---|
| ln Vivo |
PARP1-IN-44 (30 and 50 mg/kg, epidermis, once daily for 14 days) showed antitumor efficacy against CT26 tumors in BALB/c mice [1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: HCC1937 cells Tested Concentrations: 2.5, 5, 10 μM Incubation Duration: 48 h Experimental Results: Induced apoptosis in a concentration dependent manner, with apoptosis rates of 37.14 % and 62.64 % at concentrations of 5 μM and 10 μM. RT-PCR[1] Cell Types: CT26 cells Tested Concentrations: 0.25, 0.5, 1 and 2 μM Incubation Duration: 72 h Experimental Results: Increased in the expression of immune-related genes (IFN-β and CXCL10). Immunofluorescence[1] Cell Types: H2O2 (600 μM, 30 min)-induced HCC1937 cells Tested Concentrations: 1 μM Incubation Duration: 72 h Experimental Results: Decreased fluorescence intensity of PAR (green) compared to the H2O2-induced group. Increased γH2AX (green) fluorescence intensity in a concentration dependent manner. |
| Animal Protocol |
Animal/Disease Models: Six-week-old female BALB/c mice subcutaneously inoculated with CT26 cells in the axillary region[1].
Doses: 30 mg/kg and 50 mg/kg Route of Administration: Oral gavage, once daily for 14 days Experimental Results: Significantly reduced both tumor volume and weight, with the 30 mg/kg dose group exhibiting comparable tumor inhibition efficacy to RBN-2397 (30 mg/kg, p.o.). Demonstrated remarkable antitumor effects with approximately 5-fold reduction in average tumor volume and approximately 943 mg decrease in tumor weight at 50 mg/kg dose group compared to the control group. Had no significant differences in body weight changes. Displayed pronounced morphological changes (H&E staining): chromatin condensation, nuclear fragmentation, nuclear envelope rupture, increased and enlarged cytoplasmic vacuolation, loose cellular arrangement, and reduced intercellular connections. Promoted the infiltration of CD8+ T cells in the tumor microenvironment. |
| References |
| Molecular Formula |
C27H22F2N4O4S
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|---|---|
| Molecular Weight |
536.55
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| Appearance |
Typically exists as solids at room temperature
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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 | 1.8638 mL | 9.3188 mL | 18.6376 mL | |
| 5 mM | 0.3728 mL | 1.8638 mL | 3.7275 mL | |
| 10 mM | 0.1864 mL | 0.9319 mL | 1.8638 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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