| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| ln Vitro |
Imetestat is a telomerase inhibitor that can cause cancer cells to lose their ability to maintain telomere length, thereby inhibiting cell proliferation[1]. Imetestat (1.8-7.5 μM; 2-7 days) can inhibit the proliferation of CD34+ cells in primary myelofibrosis and induce apoptosis, but has no significant effect on normal umbilical cord blood CD34+ cells[2].
|
|---|---|
| ln Vivo |
Imetesta (5-30 mg/kg; intraperitoneal injection; 3 times a week; 4-8 weeks) had a dose-dependent mild inhibitory effect on normal hematopoietic stem cells in NSG mice irradiated with sublethal doses, with the 30 mg/kg dose causing the most significant reduction in normal hCD34+ cells [2].
|
| Cell Assay |
Apoptosis analysis [2]
Cell Types: Myelofibrosis CD34+ cells; Umbilical cord blood CD34+ cells Tested Concentrations: 7.5 μM Incubation Duration: 2 days Experimental Results: No apoptosis was induced in umbilical cord blood CD34+ cells; increased percentage of MF CD34+ Annexin V+ PI- cells. |
| Animal Protocol |
Animal/Disease Models:NOD/SCID/IL2Rgnull (NSG) (8 to 9 weeks old; sublethal dose irradiation) [2]
Doses: 5 mg/kg; 15 mg/kg; 30 mg/kg Route of Administration: Intraperitoneal injection; 3 times a week; for 4 or 8 weeks Experimental Results: After 8 weeks of continuous administration at a dose of 15 mg/kg, the number of hCD34+ cells decreased by 15.4%. After 8 weeks of continuous administration at a dose of 30 mg/kg, no significant decrease in the number of hCD45+ or hCD34+ cells was observed. |
| References |
| Molecular Weight |
4610.00
|
|---|---|
| CAS # |
868169-64-6
|
| Appearance |
White to off-white solid
|
| SMILES |
[Imetelstat]
|
| Synonyms |
GRN163L
|
| 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 (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
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 | 0.2169 mL | 1.0846 mL | 2.1692 mL | |
| 5 mM | 0.0434 mL | 0.2169 mL | 0.4338 mL | |
| 10 mM | 0.0217 mL | 0.1085 mL | 0.2169 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
