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| Targets |
POL1-IN-1 targets RNA polymerase I (POL1), the enzyme responsible for the transcription of ribosomal RNA (rRNA) genes. By inhibiting POL1, the compound blocks rRNA synthesis, which in turn prevents ribosome biogenesis. This disruption of protein synthesis machinery leads to reduced cell proliferation and is being explored as a therapeutic strategy in oncology.
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| ln Vitro |
POL1-IN-1 demonstrates potent in vitro inhibition of RNA polymerase I with an IC50 of less than 0.5 μM. It effectively inhibits POL1 transcription in A375 malignant melanoma cells without affecting polymerase II. The compound's selectivity for POL1 over POL2 makes it a valuable tool for studying ribosome biogenesis and cancer biology.
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| ln Vivo |
In vivo activity of POL1-IN-1 has been suggested by its potent in vitro inhibition of POL1 and its effects on ribosome biogenesis. The compound is used in cancer research to explore replication stress responses, DNA repair pathways, and synthetic lethality strategies. Further in vivo studies in animal models of cancer are needed to evaluate its antitumor efficacy and safety.
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| Enzyme Assay |
In vitro enzyme assays for POL1-IN-1 involve measuring its inhibition of RNA polymerase I transcription activity. The assay typically uses purified POL1 enzyme or nuclear extracts and measures the incorporation of radiolabeled nucleotides into rRNA transcripts in the presence of the compound. IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for POL1-IN-1 involve treating cancer cell lines (e.g., A375 melanoma cells) with varying concentrations of the compound. POL1 transcription activity is assessed by measuring rRNA synthesis using qRT-PCR or metabolic labeling. Cell proliferation is evaluated using MTT or other viability assays. The compound's selectivity for POL1 over POL2 is confirmed by measuring POL2 activity.
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| Animal Protocol |
In vivo animal experiments for POL1-IN-1 would typically involve administering the compound to tumor-bearing mouse models and evaluating efficacy by measuring tumor growth inhibition, rRNA synthesis, and ribosome biogenesis markers. The compound's potential for synthetic lethality in POL1-dependent tumors could be assessed in appropriate models.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for POL1-IN-1 are limited. The compound has a molecular weight of 356.42 and a molecular formula of C21H20N6. Its absorption, distribution, metabolism, and excretion properties have not been fully characterized. The compound is supplied as a research-use-only chemical probe.
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| Toxicity/Toxicokinetics |
Toxicological data for POL1-IN-1 are limited. As a research compound, comprehensive toxicological studies have not been reported. The compound is intended for research use only and is not for human therapeutic application. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
POL1-IN-1 (CAS#: 1822358-25-7) has the molecular formula C21H20N6 and a molecular weight of 356.42. It is a potent and selective RNA polymerase I inhibitor with an IC50 of less than 0.5 μM. The compound inhibits POL1 transcription in A375 melanoma cells without affecting POL2. It is used in cancer research.
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| Molecular Formula |
C21H20N6
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| Molecular Weight |
356.42
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| Exact Mass |
356.175
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| CAS # |
1822358-25-7
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| PubChem CID |
118509873
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| Appearance |
Solid powder
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| LogP |
3.487
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
27
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| Complexity |
591
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@H]1CN(C[C@@H](N1)C)C2=NC3=C(C=C2)C=C(C4=NC5=CC=CC=C5N34)C#N
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| InChi Key |
BUQDEURXPZKMSY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H20N6/c1-2-7-16(8-3-1)17-15-18(21-22-11-14-27(21)25-17)23-19-9-6-10-20(24-19)26-12-4-5-13-26/h1-3,6-11,14-15H,4-5,12-13H2,(H,23,24)
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| Chemical Name |
6-phenyl-N-(6-pyrrolidin-1-ylpyridin-2-yl)imidazo[1,2-b]pyridazin-8-amine
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| Synonyms |
POL1-IN-1
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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) |
DMSO : ~25 mg/mL (~70.1 mM)
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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 | 2.8057 mL | 14.0284 mL | 28.0568 mL | |
| 5 mM | 0.5611 mL | 2.8057 mL | 5.6114 mL | |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8057 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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