| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, primarily as quantitative tracers during drug development. Studies involving the use of deuterium-labeled drugs in humans have shown that these compounds may have certain advantages over their non-deuterated counterparts. Deuterated drugs have attracted attention due to their potential to affect the pharmacokinetic and metabolic profiles of drugs. Deuttetrabenazine is the first deuterated drug approved by the United States Food and Drug Administration. Deuttetrabenazine is indicated for the treatment of chorea associated with Huntington's disease as well as tardive dyskinesia. Ongoing clinical trials indicate that many other deuterated compounds are being evaluated for use as treatments for human diseases, rather than just as research tools. [1] Irinotecan hydrochloride is a topoisomerase I inhibitor. Irinotecan hydrochloride inhibits the growth of LoVo and HT-29 cells with IC50 of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and induces similar numbers of cleavable complexes in LoVo and HT-29 cells[3]. Irinotecan hydrochloride inhibits the proliferation of human umbilical vein endothelial cells (HUVEC) with IC50 of 1.3 μM[4].
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| ln Vivo |
Daily intratumoral injection of Irinotecan hydrochloride (CPT-11 hydrochloride, 5 mg/kg) for two weeks significantly inhibited tumor growth in rats, an effect also produced by continuous intraperitoneal infusion of osmotic minipumps into mice . However, Irinotecan hydrochloride (10 mg/kg) had no effect on intra-abdominal tumor growth [2]. Irinotecan hydrochloride (CPT-11, 100-300 mg/kg, ip) significantly inhibited tumor growth in HT-29 xenografts from athymic female mice on day 21. Irinotecan hydrochloride (125 mg/kg) plus TSP-1 (10 mg/kg daily) or Irinotecan hydrochloride (150 mg/kg) plus TSP-1 (20 mg/kg daily) were almost equally effective, inhibiting tumor growth by 84% and 84%, respectively. 89%, the combination is more effective than Irinotecan hydrochloride alone at doses of 250 and 300 mg/kg [4].
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| References |
|
| Molecular Formula |
C33H34D5CLN4O6
|
|---|---|
| Molecular Weight |
628.17
|
| CAS # |
718612-73-8
|
| Appearance |
Typically exists as solid at room temperature
|
| Synonyms |
Irinotecan-d5 hydrochloride; (+)-Irinotecan-d5 hydrochloride; CPT-11-d5 hydrochloride; VAL-413-d5
|
| 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 |
| 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) |
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
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|---|---|
| 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 | 1.5919 mL | 7.9596 mL | 15.9193 mL | |
| 5 mM | 0.3184 mL | 1.5919 mL | 3.1839 mL | |
| 10 mM | 0.1592 mL | 0.7960 mL | 1.5919 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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