| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
IC50: 5 nM (SAMDC)[1]
The primary target of Sardomozide HCl is S-adenosylmethionine decarboxylase (SAMDC), a key enzyme in the polyamine biosynthesis pathway. SAMDC catalyzes the decarboxylation of S-adenosylmethionine (SAM) to form decarboxylated SAM, which is then used as an aminopropyl donor for the synthesis of spermidine and spermine from putrescine. By inhibiting SAMDC, Sardomozide HCl reduces the intracellular levels of polyamines, which are essential for cell growth, differentiation, and survival. The compound has an IC50 of 5 nM in cell-based assays. |
|---|---|
| ln Vitro |
An IC50 of 5 nM was observed in a cell experiment for the S-adenosylmethionine decarboxylase (SAMDC) inhibitor sardomozide. After being treated with 3 μM Sardomozide for 48 hours, intracellular SAMDC activity drops to 10% of the control level[1]. Vacuole production is not seen in CHO/664 cells grown in the presence of Sardomozide and treated with DENSPM; instead, the cells exhibit growth inhibition and DENSPM levels comparable to those of the original CHO cells[2].
In vitro, Sardomozide HCl is a potent inhibitor of SAMDC with an IC50 of 5 nM in cell-based assays. Following treatment for 48 hours with 3 µM Sardomozide, intracellular SAMDC activity is reduced to 10% of control levels. The compound exhibits broad-spectrum antiproliferative activity against various cancer cell lines. Its mechanism of action involves the depletion of polyamines, leading to cell cycle arrest and inhibition of tumor cell proliferation. Sardomozide HCl is a second-generation polyamine synthesis inhibitor, designed to overcome the limitations of first-generation inhibitors. |
| ln Vivo |
In vivo, Sardomozide HCl has demonstrated antitumor activity in various preclinical models. As a SAMDC inhibitor, it reduces polyamine levels in tumors, leading to inhibition of tumor growth. The compound has been evaluated for its efficacy in combination with other anticancer agents. Specific in vivo efficacy data, including dosing regimens and tumor types, is not detailed in the provided search results. Further studies are needed to fully characterize its in vivo activity and therapeutic potential.
|
| Enzyme Assay |
The in vitro activity of Sardomozide HCl is assessed using cell-free SAMDC enzyme activity assays. Recombinant SAMDC is incubated with its substrate, S-adenosylmethionine (SAM), in the presence of varying concentrations of Sardomozide HCl. The production of decarboxylated SAM is measured, typically using radiolabeled substrates or by detecting the release of CO2. The IC50 is determined from dose-response curves. For cellular assays, cancer cell lines are treated with Sardomozide HCl, and intracellular polyamine levels are measured by HPLC or LC-MS/MS to confirm target engagement.
|
| Cell Assay |
The parent CHO cell line is chronically exposed to increasing
levels of Sardomozide for at least eight passages beginning at 0.1 μM.
Cell lines are serially exposed to increasing concentrations until a
panel of sublines is obtained resistant to 1 (CHO/1). 3 (CHO/3), 10
(CHO/10), 30 (CHO/30), and 100 (CHO/100) μM Sardomozide for comparative
studies[2].
|
| Animal Protocol |
In vivo, Sardomozide HCl is typically administered intraperitoneally or intravenously to mice bearing human tumor xenografts. Doses typically range from 10-100 mg/kg administered daily or every other day. Tumor growth is monitored by measuring tumor volume. At the end of the study, tumors are excised and analyzed for polyamine levels, cell proliferation (Ki-67 staining), and apoptosis (TUNEL staining). Pharmacokinetic studies involve measurement of Sardomozide HCl levels in plasma and tissues by LC-MS/MS.
|
| ADME/Pharmacokinetics |
Sardomozide HCl has a molecular weight and formula consistent with its chemical structure. The compound is soluble in water and DMSO. It should be stored as a powder at -20°C under desiccated conditions. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results. The compound's hydrochloride salt form enhances its aqueous solubility for pharmaceutical applications.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for Sardomozide HCl is not available in the provided search results. As a polyamine synthesis inhibitor, it may affect normal cell proliferation in rapidly dividing tissues, potentially leading to myelosuppression, gastrointestinal effects, or alopecia. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required to establish its full safety profile.
|
| References |
|
| Additional Infomation |
Sardomozide HCl is a research compound that was developed as a second-generation SAMDC inhibitor for cancer therapy. It is not approved for clinical use and is intended for research purposes only. The compound is a valuable tool for studying the role of polyamine metabolism in cancer cell proliferation and for exploring the therapeutic potential of targeting the polyamine biosynthesis pathway. Its development represents an advance over first-generation polyamine synthesis inhibitors.
|
| Molecular Formula |
C11H16CL2N6
|
|---|---|
| Molecular Weight |
230.26906
|
| Exact Mass |
302.081
|
| CAS # |
138794-73-7
|
| Related CAS # |
Sardomozide;149400-88-4
|
| PubChem CID |
10402702
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
490.6±55.0 °C at 760 mmHg
|
| Flash Point |
250.5±31.5 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.768
|
| LogP |
-0.49
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
19
|
| Complexity |
368
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1C/C(=N\N=C(N)N)/C2=C1C(=CC=C2)C(=N)N.Cl.Cl
|
| InChi Key |
UHEIPGJSFDAPIC-NENXIMLWSA-N
|
| InChi Code |
InChI=1S/C11H14N6.2ClH/c12-10(13)8-3-1-2-7-6(8)4-5-9(7)16-17-11(14)15/h1-3H,4-5H2,(H3,12,13)(H4,14,15,17)2*1H/b16-9+
|
| Chemical Name |
(E)-2-(4-carbamimidoyl-2,3-dihydro-1H-inden-1-ylidene)hydrazinecarboximidamide dihydrochloride
|
| Synonyms |
CGP 48664 SAM-486ACGP-48664 SAM486A CGP48664 SAM 486A
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~10 mg/mL (~32.98 mM)
H2O : ~3.85 mg/mL (~12.70 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: 1 mg/mL (3.30 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 10.0 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. View More
Solubility in Formulation 3: ≥ 1 mg/mL (3.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3427 mL | 21.7136 mL | 43.4273 mL | |
| 5 mM | 0.8685 mL | 4.3427 mL | 8.6855 mL | |
| 10 mM | 0.4343 mL | 2.1714 mL | 4.3427 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
COA