| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Additional Infomation |
CGC-11047 is a polyamine analog designed to halt cell growth and induce apoptosis.
Polyamine Analogue PG11047 is a second generation polyamine analogue, synthesized through the restriction of molecular conformations of parent polyamine compounds, with potential antineoplastic activity. Polyamine analogue PG11047 may displace endogenous polyamines from DNA binding sites, thereby interfering with cell cycle processes dependent upon polyamine binding and function, and resulting in cell-cycle arrest, induction of apoptosis, depletion of polyamines, and interference with gene and ligand-receptor activities involved with cell growth. This agent may exhibit decreased toxicity and enhanced cytotoxicity profiles compared to first-generation polyamine compounds. In tumor cells, there is an increase dependence on polyamines as well as a dysregulated polyamine metabolic pathway resulting in abnormal or sustained tumor growth. Drug Indication Investigated for use/treatment in lymphoma (unspecified), macular degeneration, prostate cancer, and solid tumors. Mechanism of Action The mechanism of action of CGC-11047 is unknown but it is believed to block the growth of cancer cells by blocking the production of new DNA in the cancer cells. Pharmacodynamics CGC-11047 is a polyamine analog with anti-proliferative properties. Polyamines are cell components considered essential for cell proliferation and differentiation. They are believed to work by displacing polyamines from their natural binding sites and preventing cell replication. CGC-11047 has been very well-tolerated in Phase I clinical trials and has demonstrated promising activity in patients with advanced disease. |
|---|
| Molecular Formula |
C14H32N4.4[HCL]
|
|---|---|
| Molecular Weight |
402.27444
|
| Exact Mass |
256.263
|
| CAS # |
206991-64-2
|
| Related CAS # |
PG-11047;308145-19-9
|
| PubChem CID |
9822383
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
0.888g/cm3
|
| Boiling Point |
367.5ºC at 760mmHg
|
| Flash Point |
178.3ºC
|
| LogP |
2.284
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
22
|
| Complexity |
153
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCNCCCNC/C=C\CNCCCNCC.Cl.Cl.Cl.Cl
|
| InChi Key |
MNJCMBNLXQCNHO-YGGCHVFLSA-N
|
| 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-;;;;
|
| Chemical Name |
(Z)-N,N'-bis[3-(ethylamino)propyl]but-2-ene-1,4-diamine;tetrahydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ≥ 30 mg/mL (~74.58 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
