| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
When treated to Intoplicine for 1 hour at final doses of 2.5 μg/mL and 10.0 μg/mL, 26% and 54% of evaluable samples showed a positive in vitro response, respectively [2]. During continuous exposure to Intoplicine at doses of 0.25 μg/mL and 2.5 μg/mL, 16% and 71% of evaluable samples showed positive reactions, respectively [2]. Activity against breast (71%), non-small cell lung cancer (69%), and ovarian cancer (45%) cancer colony-forming units was seen after 1 hour of exposure to Intoplicine at a dosage of 10.0 μg/mL [2].
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|---|---|
| ln Vivo |
At the highest nontoxic dose (HNTD) (6 mg/kg/injection, total dose 36 mg/kg), Intoplicine demonstrated high activity with a T/C of 0%, equating to a total log cell death of 3[ 3].
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| References |
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| Additional Infomation |
Intoplicine is a pyridoindole.
Intoplicine has been used in trials studying the treatment of Unspecified Adult Solid Tumor, Protocol Specific. Intoplicine is a benzopyridoindole derivative with antineoplastic property. Intoplicine inhibits activities of both topoisomerase I and II via intercalating DNA helix, thereby hindering the movements of enzymes along DNA molecules during DNA transcription and replication, respectively. Furthermore, this agent stabilizes DNA-enzyme complexes during unwinding processes by both topoisomerases, leading to double- and single-stranded DNA breaks. Consequently, these effects bring about cell growth inhibition and apoptosis of tumor cells. |
| Molecular Formula |
C21H24N4O
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|---|---|
| Molecular Weight |
348.45
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| Exact Mass |
348.195
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| CAS # |
125974-72-3
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| Related CAS # |
Intoplicine dimesylate;133711-99-6
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| PubChem CID |
65954
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| Appearance |
White to off-white solid powder
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| Density |
1.286g/cm3
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| Boiling Point |
635.5ºC at 760mmHg
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| Flash Point |
338.2ºC
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| Vapour Pressure |
9.55E-17mmHg at 25°C
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| Index of Refraction |
1.755
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| LogP |
4.319
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
473
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QROONAIPJKQFMC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H24N4O/c1-13-12-23-21(22-9-4-10-25(2)3)19-18-16-7-6-15(26)11-14(16)5-8-17(18)24-20(13)19/h5-8,11-12,24,26H,4,9-10H2,1-3H3,(H,22,23)
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| Chemical Name |
16-[3-(dimethylamino)propylamino]-13-methyl-11,15-diazatetracyclo[8.7.0.02,7.012,17]heptadeca-1(10),2(7),3,5,8,12(17),13,15-octaen-5-ol
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| Synonyms |
RP-60475; NSC-D-645008; Intoplicine
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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 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)
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| Solubility (In Vitro) |
DMSO : ~80 mg/mL (~229.59 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (5.74 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 20.0 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: ≥ 2 mg/mL (5.74 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 20.0 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: ≥ 2 mg/mL (5.74 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 | 2.8699 mL | 14.3493 mL | 28.6985 mL | |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7397 mL | |
| 10 mM | 0.2870 mL | 1.4349 mL | 2.8699 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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