| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PARP1/ERK IN-1 (I-16) (7 days) can inhibit the proliferation of various cancer cell lines. Its IC50 values against HCT116, HT29, CFPAC-1 and W1990 cells are 0.41 μM, 2.58 μM, 5.51 μM and 2.13 μM, respectively, and it has very low toxicity to normal MCF-10A and AML-12 cells [1]. PARP1/ERK IN-1 (0.25-1 μM; 7 days) reduces the protein levels of PARP1 and p-ERK1/2 in HCT116 cells in a concentration-dependent manner and impairs their DNA repair pathway [1]. PARP1/ERK IN-1 (100 μM; 6-8 hours) can directly bind to PARP1 and ERK proteins in HCT116 cell lysate and improve their thermal stability [1]. PARP1/ERK IN-1 (0.25–1 μM; 0–14 days) inhibited long-term colony formation of HCT116 cells in a dose-dependent manner and suppressed the directed migration of HCT116 cells[1]. PARP1/ERK IN-1 (0.25–1 μM; 7 days) induced apoptosis of HCT116 cells in a dose-dependent manner, arrested the cell cycle at the G2/M phase, and induced significant DNA damage[1].
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| ln Vivo |
PARP1/ERK IN-1 (5-20 mg/kg; intraperitoneal injection; once daily; 21 days) inhibited the growth of colorectal cancer tumors in a dose-dependent manner in the HCT116 xenograft mouse model [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: HCT116 Tested Concentrations: 0.25, 0.5, 1 μM Incubation Duration: 7 days Experimental Results: Concentration-dependently reduced the protein levels of PARP1, p-ERK1/2, p-p90RSK1, BRCA1 and Rad51, while increasing the protein level of γH2AX. |
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (male, 6 weeks old, 18-22 g, HCT116 cell xenograft) [1]
Doses: 5 mg/kg; 10 mg/kg; 20 mg/kg Route of Administration: Intraperitoneal injection; once daily for 21 days Experimental Results: The tumor growth inhibition rate (TGI) in the 20 mg/kg dose group reached 57.7%, which was superior to olaparib (50 mg/kg, TGI=37.0%) and BVD-523 (5 mg/kg, TGI=45.8%), and comparable to the combination of olaparib and BVD-523 (TGI=54.2%). No significant weight loss was observed in any of the treatment groups. Ki-67 expression was reduced in tumor tissue in the 20 mg/kg group, indicating that tumor cell proliferation was inhibited. The expression of BRCA1 and Rad51 was decreased in tumor tissues of the 20 mg/kg group. The fluorescence signal intensity of PARP1 and p-ERK1/2 was significantly decreased in tumor tissues of the 20 mg/kg group. |
| References |
| Molecular Formula |
C23H19FN8O2
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|---|---|
| Molecular Weight |
458.45
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(NC1=CC2=C(C=N1)C(C3=CC=C(C=C3)F)=NN2)N[C@@H](C4=NC5=C(N4)C=CC=C5C(N)=O)C
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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 | 2.1813 mL | 10.9063 mL | 21.8126 mL | |
| 5 mM | 0.4363 mL | 2.1813 mL | 4.3625 mL | |
| 10 mM | 0.2181 mL | 1.0906 mL | 2.1813 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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