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| Targets |
The primary target of CGC-11047 is the polyamine pathway. As a polyamine analogue, it acts as a nonfunctional competitor of spermine. It is thought to displace endogenous polyamines from their binding sites on DNA and other molecules. By interfering with the normal function of polyamines, which are crucial for cell cycle progression, CGC-11047 disrupts cell growth and proliferation, leading to cell cycle arrest and apoptosis.
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| ln Vitro |
In vitro, CGC-11047 has been shown to have broad-spectrum anticancer activity. As a polyamine analogue, it is designed to halt cell growth and induce apoptosis in tumor cells. Its mechanism involves displacing natural polyamines from DNA binding sites, thereby interfering with cell cycle progression. Studies have demonstrated its ability to inhibit the growth of various cancer cell lines, confirming its potential as an antineoplastic agent.
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| ln Vivo |
In vivo, CGC-11047 has demonstrated antitumor activity in animal models. As a second-generation polyamine analogue, it was designed to have improved pharmacological properties and efficacy compared to first-generation compounds. Its in vivo activity is a result of its ability to disrupt polyamine metabolism in tumor cells, leading to growth inhibition and tumor regression. The compound has been studied for its potential to treat various cancers.
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| Enzyme Assay |
The in vitro activity of CGC-11047 is typically assessed using cell proliferation and viability assays. In a standard protocol, cancer cells are seeded in 96-well plates and treated with increasing concentrations of CGC-11047 for a period (e.g., 48-72 hours). Cell viability is then measured using a colorimetric assay, such as MTT or CellTiter-Glo. The half-maximal inhibitory concentration (IC50) is calculated to quantify the compound's potency.
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| Cell Assay |
For in vitro cellular studies, CGC-11047 is typically dissolved in water, as it is a hydrochloride salt with high aqueous solubility (≥30 mg/mL). Cells are seeded in appropriate culture media and allowed to adhere. They are then treated with serial dilutions of the compound. After incubation, the effects on cell cycle distribution and apoptosis are assessed using flow cytometry. The compound's ability to displace polyamines can also be studied in these cellular models.
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| Animal Protocol |
The in vivo efficacy of CGC-11047 is evaluated in xenograft mouse models. In these studies, human tumor cells are implanted subcutaneously into immunodeficient mice. When tumors reach a certain size, the animals are treated with CGC-11047, typically via intraperitoneal or intravenous injection. Tumor growth is monitored by caliper measurements, and tumor weights are assessed at the end of the study. The compound's ability to inhibit tumor growth and induce regression is then evaluated.
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| ADME/Pharmacokinetics |
Dosing in animal models typically involves intraperitoneal or intravenous administration. The compound is formulated in a suitable vehicle, such as saline or a buffer, for injection. For pharmacokinetic studies, blood samples are collected at various time points, and plasma concentrations of CGC-11047 are measured. These studies help determine the compound's bioavailability, half-life, and distribution. The compound has a molecular formula of C14H36Cl4N4.
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| Toxicity/Toxicokinetics |
The toxicity profile of CGC-11047 is a critical aspect of its development as an anticancer agent. As a polyamine analogue, its toxicity is related to its interference with essential cellular processes. Standard toxicology studies in animals are conducted to determine its maximum tolerated dose (MTD) and identify any dose-limiting toxicities. These studies are essential for establishing a safe starting dose for clinical trials.
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| Additional Infomation |
CGC-11047 is a polyamine analog designed to inhibit cell growth and induce apoptosis. The polyamine analog PG11047 is a second-generation polyamine analog with potential antitumor activity by restricting the conformational synthesis of the parent polyamine compound. PG11047 can displace endogenous polyamines from their DNA binding sites, thereby interfering with polyamine-dependent cell cycle processes, leading to cell cycle arrest, apoptosis induction, polyamine depletion, and interference with gene and ligand-receptor activity related to cell growth. Compared to first-generation polyamine compounds, this drug may exhibit lower toxicity and stronger cytotoxicity. Increased polyamine dependence and dysregulation of polyamine metabolic pathways in tumor cells lead to abnormal or persistent tumor growth. Drug Indications It has been investigated for the treatment of lymphoma (not specified), macular degeneration, prostate cancer, and solid tumors. Mechanism of Action The mechanism of action of CGC-11047 is not fully understood, but it is believed to block cancer cell growth by inhibiting the production of new DNA in cancer cells. Pharmacodynamics CGC-11047 is a polyamine analog with anti-proliferative properties. Polyamines are cellular components and are considered essential for cell proliferation and differentiation. It is believed that CGC-11047's mechanism of action involves displacing polyamines from their native binding sites, thereby preventing cell replication. CGC-11047 was well-tolerated in a Phase I clinical trial and showed good efficacy in patients with advanced disease.
CGC-11047, also known as PG-11047 tetrahydrochloride, is a second-generation polyamine analogue and a nonfunctional competitor of spermine. It has broad-spectrum anticancer activities and has been investigated for its potential as an antineoplastic agent. As a research compound, it represents a strategy to target polyamine metabolism in cancer therapy. It is not an approved drug but has been studied in preclinical and early clinical settings. |
| Molecular Formula |
C14H32N4.4[HCL]
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| Molecular Weight |
402.27444
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| Exact Mass |
256.263
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| CAS # |
206991-64-2
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| Related CAS # |
PG-11047;308145-19-9
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| PubChem CID |
9822383
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| Appearance |
Off-white to light yellow solid powder
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| Density |
0.888g/cm3
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| Boiling Point |
367.5ºC at 760mmHg
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| Flash Point |
178.3ºC
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| LogP |
2.284
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
22
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| Complexity |
153
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCNCCCNC/C=C\CNCCCNCC.Cl.Cl.Cl.Cl
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| InChi Key |
MNJCMBNLXQCNHO-YGGCHVFLSA-N
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| InChi Code |
InChI=1S/C14H32N4.4ClH/c1-3-15-11-7-13-17-9-5-6-10-18-14-8-12-16-4-2;;;;/h5-6,15-18H,3-4,7-14H2,1-2H3;4*1H/b6-5-;;;;
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| Chemical Name |
(Z)-N,N'-bis[3-(ethylamino)propyl]but-2-ene-1,4-diamine;tetrahydrochloride
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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) |
H2O : ≥ 30 mg/mL (~74.58 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 | 2.4859 mL | 12.4295 mL | 24.8589 mL | |
| 5 mM | 0.4972 mL | 2.4859 mL | 4.9718 mL | |
| 10 mM | 0.2486 mL | 1.2429 mL | 2.4859 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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