| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PARP1-IN-50 (Compound 13) showed significant antiproliferative activity in HCC-1937, Capan-1, MCF-7 and PANC-1 cells, with IC50 values of 0.88, 0.56, 4.49 and 1.53 μM, respectively [1]. PARP1-IN-50 (1-10 μM, 48 h) induced G2/M phase arrest in HCC-1937 cells and inhibited the expression levels of CDK1 and cyclin B [1]. PARP1-IN-50 (1-10 μM, 4 h) inhibited H2O2-induced PAR formation in HCC-1937 cells [1]. PARP1-IN-50 (1-10 μM, 30 mins) increased PARP-1-DNA capture in HCC-1937 cells and induced DNA double-strand breaks [1]. PARP1-IN-50 (1-10 μM, 48 h) induced apoptosis in HCC-1937 cells [1].
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|---|---|
| ln Vivo |
PARP1-IN-50 (Compound 13) (25-50 mg/kg, lateral wall, once daily for 21 days) significantly inhibited the growth of HCC-1937 xenograft tumors in BALB/c nude mice and had a good safety profile [1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HCC-1937, Capan-1, MCF-7, PANC-1, A549, H460, CaCo-2, HL-7702 Tested Concentrations: 20 μM Incubation Duration: 48 h Experimental Results: Showed an inhibition rate of 100% in SK-OV-3 cells, 84.36% in PANC-1, 44.68% in H460 cells, 75.89 % in HL-7702 cells and 68.33% in MCF-7 cells. Western Blot Analysis[1] Cell Types: HCC-1937 cells Tested Concentrations: 1, 5 and 10 μM Incubation Duration: 0.5, 4 and 48 h Experimental Results: Inhibited PAR levels and increased the PARP-1-DNA trapping levles. Increased γ-H2AX protein levels. Reduced CDK1 and cyclin B levles. Upregulated the expression of Bax and downregulated the expression of Bcl-2. |
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice with HCC-1937 xenograft (female, 5-6 weeks, 18-22 g )[1]
Doses: 25 mg/kg, 50 mg/kg Route of Administration: Orally administration Experimental Results: Showed growth inhibition rates of 53.5% and 71.4% at 25 mg/kg and 50 mg/kg. Reduced tumor weight and volume. Had no significant changes in body weight and no significant organ toxicity. Reduced Ki67 expression and increased γ-H2AX expression. |
| References |
| Molecular Formula |
C22H26BR2N6O4S2
|
|---|---|
| Molecular Weight |
662.42
|
| CAS # |
2255341-36-5
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| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 1.5096 mL | 7.5481 mL | 15.0962 mL | |
| 5 mM | 0.3019 mL | 1.5096 mL | 3.0192 mL | |
| 10 mM | 0.1510 mL | 0.7548 mL | 1.5096 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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