Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
PARP-1 ( IC50 = 14.7 nM ); PARP-2 ( IC50 = 0.9 μM )
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ln Vitro |
In a dose-dependent way, PARP1-IN-5 (0.1~10 μM) can markedly increase the cytotoxicity of CBP on A549 cells. In SK-OV-3 cells, PARP1-IN-5 (0.1~10 μM) reduces MCM2-7 expression. There are minimal cytotoxic effects of PARP1-IN-5 (0.1~320 μM) on A549 cells. SK-OV-3 cells, or PARP1-IN-5, have the ability to dramatically lower the PAR level[1]. Through PARP-1, PARP1-IN-5 has anticancer effects. PARP1-IN-5 may elevate the expression of γ-H2AX [1].
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ln Vivo |
The results of PARP1-IN-5 (1000 mg/kg; po) indicate that there is no statistically significant variation in blood routine or body weight[1]. The inhibitory impact of 50 mg/kg of carboplatin on A549 cells is greatly enhanced by PARP1-IN-5 (25 and 50 mg/kg; po; 12 days)[1]. There is a favorable correlation between the expression of PARP-1 and PARP1-IN-5 (50 mg/kg; po)[1]. It is possible for PARP1-IN-5 to downregulate PAR expression while upregulating γ-H2AX expression[1].
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Animal Protocol |
Animal/Disease Models: Mice[1]
Doses: 1000 mg/kg Route of Administration: Po Experimental Results: There was no significant difference in the body weight and blood routine. Animal/Disease Models: Mice[1] Doses: 25 and 50 mg/kg Route of Administration: Po; 12 days Experimental Results: Dramatically enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg. Animal/Disease Models: Male Sprague−Dawley (SD) rats[1] Doses: 50 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Po; 12 days Experimental Results: Positively correlated with the expression of PARP-1. |
References |
[1]. Long H, et al. Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer. J Med Chem. 2021;64(16):12089-12108.
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Molecular Formula |
C25H24N2O5S
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Molecular Weight |
464.53
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CAS # |
2735645-53-9
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Related CAS # |
PARP1-IN-5 dihydrochloride;2823308-89-8
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Synonyms |
PARP1-IN-5
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1527 mL | 10.7636 mL | 21.5271 mL | |
5 mM | 0.4305 mL | 2.1527 mL | 4.3054 mL | |
10 mM | 0.2153 mL | 1.0764 mL | 2.1527 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.