| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 11.56 μM (IL6/STAT3 signaling pathway), 3.32 μM (MDA-MB-231), 4.72 μM (H4), 3.14 μM (HepG2)[1]
Angoline targets the IL-6/STAT3 signaling pathway, specifically inhibiting STAT3 phosphorylation and downstream signaling. STAT3 (signal transducer and activator of transcription 3) is a transcription factor that is activated by phosphorylation in response to cytokines such as IL-6 and growth factors. Once phosphorylated, STAT3 dimerizes and translocates to the nucleus, where it regulates the expression of genes involved in cell proliferation, survival, angiogenesis, and immune evasion. Constitutive STAT3 activation is a hallmark of many cancers and is associated with poor prognosis. Angoline inhibits STAT3 phosphorylation (IC₅₀ = 11.56 μM), blocking its nuclear translocation and target gene expression. The compound is specific for the IL-6/STAT3 pathway. |
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| ln Vitro |
The STAT3, STAT1, and NF-κB signaling pathways are inhibited by angoline (0-100 μM; 1 h), with IC50 values of 11.56, >100, and >100 μM, respectively [1]. The effects of angoline (0-100 μM; 2 h) on STAT3 phosphorylation [1]. Angoline (0-100 μM; 72 h) suppresses the proliferation of HepG2, H4, and MDA-MB-231 cells [1].
In vitro studies have demonstrated that Angoline is a potent and specific inhibitor of the IL-6/STAT3 signaling pathway with an IC₅₀ of 11.56 μM. The compound inhibits STAT3 phosphorylation and its target gene expression. In cancer cell lines with constitutive STAT3 activation, Angoline treatment results in reduced cell proliferation and growth. The compound shows specificity for STAT3 over other STAT family members, minimizing off-target effects. Angoline has been used to study the role of STAT3 signaling in cancer cell survival, proliferation, and drug resistance. The compound's activity is concentration-dependent and reversible. |
| ln Vivo |
In vivo activity data for Angoline is limited in the available literature, as the compound is primarily used as a research tool in cell-based studies. The compound's potent STAT3 inhibition (IC₅₀ = 11.56 μM) suggests it could have therapeutic potential in STAT3-driven cancers. However, comprehensive in vivo efficacy studies have not been extensively reported. Future studies may explore its effects in animal models of STAT3-dependent malignancies. The compound's specificity for the IL-6/STAT3 pathway makes it a promising candidate for further investigation.
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| Enzyme Assay |
Cell-free biochemical assays for Angoline typically measure inhibition of STAT3 phosphorylation or STAT3-DNA binding. A standard protocol involves incubating recombinant STAT3 protein with varying concentrations of Angoline (0.1-100 μM) and assessing STAT3 phosphorylation using kinase assays with [γ-³²P]ATP or using phospho-specific antibodies in ELISA format. STAT3-DNA binding activity can be measured using electrophoretic mobility shift assays (EMSA) or ELISA-based DNA binding assays with STAT3-specific DNA consensus sequences. IC₅₀ values are determined from dose-response curves using nonlinear regression analysis. Assays are performed in triplicate with appropriate positive and negative controls.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HepG2/STAT3 cell line Tested Tested Concentrations: 0, 1, 10, 30 and 100 μM Incubation Duration: 2 hrs (hours) Experimental Results: Inhibited IL-6-induced phosphorylation of STAT3 in HepG2/STAT3 cells. Cell Proliferation Assay[1] Cell Types: MDA-MB-231, H4 and HepG2 cell lines Tested Tested Concentrations: 0-100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited proliferation of MDA-MB-231, H4 and HepG2 cells with IC50 values of 3.32, 4.72 and 3.14 μM, respectively. Cellular assays for Angoline typically use cancer cell lines with constitutive STAT3 activation. A standard protocol involves culturing cells (e.g., breast, prostate, or multiple myeloma cell lines) in 96-well plates, treating with Angoline at concentrations ranging from 1-100 μM for 24-72 hours. STAT3 phosphorylation is assessed by Western blotting using phospho-specific antibodies (pSTAT3-Tyr705). STAT3 target gene expression (e.g., Bcl-2, Mcl-1, Cyclin D1, VEGF) is measured by qPCR. Cell proliferation is assessed by MTT or CellTiter-Glo assays. Apoptosis is measured by caspase-3/7 activity or Annexin V staining. The compound's specificity for STAT3 over STAT1 and other STATs can be confirmed by Western blotting. |
| Animal Protocol |
In vivo studies with Angoline are limited, as the compound is primarily a research tool for in vitro applications. If conducted, a typical protocol might involve administration of Angoline to tumor-bearing mice by intraperitoneal or oral administration, followed by assessment of STAT3 phosphorylation and target gene expression in tumor tissues. Tumor growth inhibition would be monitored over 2-4 weeks. However, comprehensive in vivo efficacy studies have not been extensively reported for this compound. Future studies may explore its therapeutic potential in STAT3-driven cancers.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Angoline is limited, as the compound is primarily used in research settings. The compound's molecular weight is 379.41 g/mol. The compound's physicochemical properties suggest moderate lipophilicity. For in vivo applications, the compound would likely require formulation to enhance bioavailability. The compound is typically dissolved in DMSO for in vitro studies. Metabolism and clearance pathways have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Toxicological data specific to Angoline is limited, as the compound is a research chemical used primarily in in vitro settings. At effective concentrations (11.56 μM for STAT3 inhibition), the compound does not show significant cytotoxicity in most cell types. Higher concentrations may have off-target effects or cytotoxicity. As a STAT3 inhibitor, potential toxicity could arise from inhibition of STAT3 in tissues where the pathway is important for normal function. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
Angolin is a benzophenanthridine alkaloid. It has been reported to be found in celandine, bleaching henryi, and other organisms with relevant data.
Angoline is a research compound and not an approved drug. No clinical trials or regulatory approvals exist for this compound. It is commercially available from various suppliers for research use only. The compound's primary value lies in its utility as a pharmacological tool for studying the IL-6/STAT3 signaling pathway. With an IC₅₀ of 11.56 μM, Angoline is a potent and specific inhibitor of STAT3 phosphorylation and target gene expression, enabling researchers to investigate the roles of STAT3 signaling in cancer cell proliferation, survival, and drug resistance. |
| Molecular Formula |
C22H21NO5
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|---|---|
| Molecular Weight |
379.41
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| Exact Mass |
379.142
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| CAS # |
21080-31-9
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| Related CAS # |
Angoline hydrochloride;1071676-04-4
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| PubChem CID |
189060
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| Appearance |
White to off-white solid powder
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| Density |
1.36g/cm3
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| Boiling Point |
555.5ºC at 760 mmHg
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| Flash Point |
164.1ºC
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| Vapour Pressure |
2.23E-12mmHg at 25°C
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| Index of Refraction |
1.678
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| LogP |
4.412
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
561
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C(C2=C(C=CC(=C2OC)OC)C3=C1C4=CC5=C(C=C4C=C3)OCO5)OC
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| InChi Key |
LVWAKZBZWYHYCJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21NO5/c1-23-20-14(6-5-12-9-17-18(10-15(12)20)28-11-27-17)13-7-8-16(24-2)21(25-3)19(13)22(23)26-4/h5-10,22H,11H2,1-4H3
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| Chemical Name |
1,2,13-trimethoxy-12-methyl-13H-[1,3]benzodioxolo[5,6-c]phenanthridine
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 20.83 mg/mL (54.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.59 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.59 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6357 mL | 13.1784 mL | 26.3567 mL | |
| 5 mM | 0.5271 mL | 2.6357 mL | 5.2713 mL | |
| 10 mM | 0.2636 mL | 1.3178 mL | 2.6357 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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