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Ivospemin hydrochloride

Alias: SBP-101 hydrochloride
Ivospamine hydrochloride (SBP-101) is a spermidine analog with anticancer effects.
Ivospemin hydrochloride
Ivospemin hydrochloride Chemical Structure CAS No.: 259657-09-5
Product category: Drug Derivative
This product is for research use only, not for human use. We do not sell to patients.
Size Price
500mg
1g
Other Sizes
Official Supplier of:
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Product Description
Ivospemin (SBP-101) hydrochloride is a spermine analog with anticancer effects. Ivospemin hydrochloride has shown effects in both in vitro and in vivo in slowing the progression of pancreatic and ovarian cancers. Ivospemin hydrochloride has a moderate inducing effect on polyamine catabolism, but a stronger inhibitory effect on ornithine decarboxylase activity. Ivospemin hydrochloride holds promise for applications in cancer research.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Ivospemin hydrochloride (500 nM to 10 µM, 96 h) reduced the cell viability of human ovarian adenocarcinoma cells, with IC50 values ranging from 0.95 µM to 3.24 µM, independent of cisplatin sensitivity [2]. IC50 values of human ovarian adenocarcinoma cell lines after Ivospemin treatment [1] Cell Line CaOV-3 A2780 OV90 ACRP Ivospemin 96 h IC50 2.56 µM 0.95 µM 3.24 µM 1.41 µM
ln Vivo
Ivospemin hydrochloride (24 mg/kg, intraperitoneal injection, once every 2 weeks for 3 consecutive weeks, alternating weeks for 60 days) increased survival in a mouse model of ovarian adenocarcinoma by delaying disease effects and reducing overall tumor burden [2][3].
Cell Assay
Cell Viability Assay[2]
Cell Types: A2780, OV90, ACRP, and CaOV-3 cell lines
Tested Concentrations: 500 nM to 10 µM
Incubation Duration: 96 h
Experimental Results: Reduced cell viability in A2780, OV90, ACRP, and CaOV-3 cell lines.
Animal Protocol
Animal/Disease Models: Murine Ovarian Adenocarcinoma Model[2][3]
Doses: 24 mg/kg
Route of Administration: i.p., 2qw×3, alternating weeks for 60 days
Experimental Results: Produced a 20% increase in median survival from 43 days to 52 days post-injection, extended the time to ascites formation to 46.9 days, an increase of 13% combined with Gemcitabine or Topotecan.
References

[1]. International Nonproprietary Names for Pharmaceutical Substances (INN).

[2]. The Polyamine Analogue Ivospemin hydrochloride Increases Chemotherapeutic Efficacy in Murine Ovarian Cancer. Biomedicines. 2024 May 23;12(6):1157.

[3]. The Synergistic Benefit of Combination Strategies Targeting Tumor Cell Polyamine Homeostasis. Int J Mol Sci. 2024 Jul 26;25(15):8173.

Additional Infomation
Ivospemin Hydrochloride is the hydrochloride form of Ivospemin, an analogue of the natural polyamine (PA) with potential antitumor activity. After subcutaneous injection, Ivospemin displaces endogenous PA from its binding sites on the cell surface, thereby preventing PA internalization. This inhibits PA-dependent cell cycle progression, leading to cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. PA uptake is upregulated in various tumor types, and elevated PA levels result in enhanced tumor cell growth.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H42CL4N4O2
Molecular Weight
464.34
Exact Mass
464.203
CAS #
259657-09-5
Related CAS #
Ivospemin
PubChem CID
155676458
Appearance
Typically exists as solids at room temperature
Hydrogen Bond Donor Count
10
Rotatable Bond Count
17
Heavy Atom Count
26
Complexity
198
Defined Atom Stereocenter Count
2
SMILES
CCNCC[C@@H](CNCCCCNC[C@H](CCNCC)O)O.Cl.Cl.Cl.Cl
InChi Key
SCDBHUCANIJZED-VNMXSFETSA-N
InChi Code
InChI=1S/C16H38N4O2.4ClH/c1-3-17-11-7-15(21)13-19-9-5-6-10-20-14-16(22)8-12-18-4-2;;;;/h15-22H,3-14H2,1-2H3;4*1H/t15-,16-;;;;/m0..../s1
Chemical Name
(2S)-4-(ethylamino)-1-[4-[[(2S)-4-(ethylamino)-2-hydroxybutyl]amino]butylamino]butan-2-ol;tetrahydrochloride
Synonyms
SBP-101 hydrochloride
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 Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1536 mL 10.7680 mL 21.5359 mL
5 mM 0.4307 mL 2.1536 mL 4.3072 mL
10 mM 0.2154 mL 1.0768 mL 2.1536 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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