| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Prostat (compound 11) hydrochloride showed potent induction of the target cell differentiation marker CD11b in the THP-1 cell line with an EC50 of 7 nM; and antiproliferative activity in AML kasumi-1 cells with an EC50 of 2 nM[1]. After 4 days of treatment with prostat (compound 11) hydrochloride, GRP expression was inhibited in a dose-dependent manner at pharmacologically effective concentrations (EC50 = 3 nM, H209; 4 nM, H1417). After 12 days of treatment with prostat (compound 11) hydrochloride, small cell lung cancer (SCLC) cells showed potent antiproliferative activity (EC50 = 6 nM, H1417), which was associated with GRP expression inhibition[1].
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|---|---|
| ln Vivo |
Prodexostat (compound 11) (5 mg/kg; orally; once daily; for 30 days) hydrochloride treatment inhibited tumor growth in a patient-derived xenograft small cell lung cancer (SCLC) model [1]. Prodexostat (once daily; for 4 days) hydrochloride treatment significantly downregulated GRP mRNA levels at a dose of 2.5 mg/kg and maximally inhibited GRP expression in SCLC human tumor xenograft (H1417) mice at a dose of 5 mg/kg [1]. After intravenous injection, the systemic clearance of prodexostat (compound 11; 5 mg/kg) hydrochloride was 32.4 mL/min/kg, the elimination half-life was 2 hours, and the volume of distribution was 7.5 L/kg. After oral administration, prodexostat (compound 11; 5 mg/kg) hydrochloride was readily absorbed, with an AUC0-24h of 1.8 μM·h, a Cmax of 0.36 μM, and an oral bioavailability of 32% [1].
|
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice carrying small cell lung cancer (SCLC)[1]
Doses: 5 mg/kg Route of Administration: Oral; daily; for 30 days Experimental Results: Tumor growth inhibition rate (TGI) was 78% at a dose of 5 mg/kg, with no weight loss. |
| References |
| Molecular Formula |
C24H24CLF2N5O2
|
|---|---|
| Molecular Weight |
487.93
|
| CAS # |
1821307-11-2
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
N#CC1=CC=C(C(N=C(N2CCC(N)CC2)N3C)=C(C4=CC=C(OC)C(F)=C4)C3=O)C=C1F.Cl
|
| Synonyms |
CC-90011 hydrochloride; LSD1-IN-7 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 (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 | 2.0495 mL | 10.2474 mL | 20.4947 mL | |
| 5 mM | 0.4099 mL | 2.0495 mL | 4.0989 mL | |
| 10 mM | 0.2049 mL | 1.0247 mL | 2.0495 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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