Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
Other Sizes |
|
Targets |
Topoisomerase I Topoisomerase II
|
---|---|
ln Vitro |
After being exposed to Intoplicine dimesylate for one hour at final concentrations of 2.5 and 10.0 micrograms/mL, respectively, 26% and 54% of the assessable specimens exhibited positive in vitro responses[2]. Positive reactions were observed in 16% and 71% of the assessable specimens after continuous exposure to Intoplicine dimesylate at doses of 0.25 micrograms/mL and 2.5 micrograms/mL, respectively[2]. At 10.0 micrograms/mL of Intoplicine dimesylate, colony-forming units of breast (71%), non-small-cell lung (69%), and ovarian (45%) cancer are seen to be active[2].
|
ln Vivo |
Intoplicine dimesylate exhibits high activity with a T/C of 0% and a matching total log cell death of 3 at the highest non-toxic dosage (HNTD) of 6 mg/kg/injection, total dose, 36 mg/kg[3].
|
References |
[1]. Riou JF, et al. Intoplicine (RP 60475) and its derivatives, a new class of antitumor agents inhibiting both topoisomerase I and II activities. Cancer Res. 1993;53(24):5987-5993.
[2]. Eckardt JR, et al. Activity of intoplicine (RP60475), a new DNA topoisomerase I and II inhibitor, against human tumor colony-forming units in vitro. J Natl Cancer Inst. 1994;86(1):30-33. [3]. Bissery MC, et al. Antitumor activity of intoplicine (RP 60475, NSC 645008), a new benzo-pyrido-indole: evaluation against solid tumors and leukemias in mice. Invest New Drugs. 1993;11(4):263-277. |
Molecular Formula |
C23H32N4O7S2
|
---|---|
Molecular Weight |
540.65
|
CAS # |
133711-99-6
|
Related CAS # |
Intoplicine;125974-72-3
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
CN(CCCNc1ncc(C)c2c1c1c(n2)ccc2cc(ccc12)O)C.CS(=O)(O)=O.CS(=O)(O)=O
|
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 (e.g. under nitrogen), avoid exposure to moisture and light. |
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 : 115 mg/mL (212.71 mM)
H2O : 100 mg/mL (184.96 mM)x |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.75 mg/mL (10.64 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 57.5 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: ≥ 5.75 mg/mL (10.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 57.5 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: ≥ 5.75 mg/mL (10.64 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 | 1.8496 mL | 9.2481 mL | 18.4963 mL | |
5 mM | 0.3699 mL | 1.8496 mL | 3.6993 mL | |
10 mM | 0.1850 mL | 0.9248 mL | 1.8496 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.