| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Spiromethacin hydrochloride (0-100 μg/mL; 24 and 48 h) inhibits phospholipid non-contact colonization in a dose-dependent manner [1]. Spirolocin hydrochloride (30 μg/mL; 24 h) inhibits the MIA PaCa-2 and CFPAC-1 cells' ability to move. -1 and MIA PaCa-2 cells, considerably raising the levels of intracellular ROS [1]. In the G2 phase, spirolocin hydrochloride (10 and 20 μg/mL; 24 h) inhibits late cycle progression [2].
|
|---|---|
| ln Vivo |
In mouse MIA PaCa-2 xenografts, spirolocin hydrochloride (68 mg/kg; ip; every other day for two weeks) inhibits the formation of tumors [2].
|
| Cell Assay |
Cell viability assay[1]
Cell Types: CFPAC-1, MIA PaCa-2, HEK-293 and HL -7702 Cell Tested Concentrations: 0-100 μg/mL Incubation Duration: 24 and 48 hrs (hours) Experimental Results: CFPAC-1 and MIA PaCa- 2 Cells demonstrated time- and dose-dependent growth reduction. Exhibits low cytotoxicity to normal HEK-293 and HL-7702 cells. The IC50 of CFPAC-1 treated for 48 hrs (hours) is 15.2±2.0 μg/mL (31.5±2.0 μM), MIA PaCa-2 is 12.9±0.9 μg/mL (26.8±0.9 μM), and MIA PaCa-2 is 41.9±1.4 μg/ mL (86.9 ±1.4 μM for HEK-293) and 71.2±3.3 μg/mL (147.7±3.3 μM) for HL-7702. Apoptosis analysis[1] Cell Types: CFPAC-1 and MIA PaCa-2 Cell Tested Concentrations: 7.6 and 15.2 μg/mL for CFPAC-1 and 6.45 and 12.9 μg/mL for MIA PaCa-2 Incubation Duration: 48 hrs (hours) Experimental Results: Increase apoptotic cells early. Western Blot Analysis[1] Cell Types: CFPAC-1 and MIA PaCa-2 Cell Tested Concentrations: 10, 20 and 30 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: The amount of caspase-3/9 cleaved increased in a dose-dependent manner. The expression of Bax was up-regulated, while the expres |
| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse, MIA PaCa-2 xenograft model [2]
Doses: 68 mg/kg Route of Administration: intraperitoneal (ip) injection every other day for two weeks Experimental Results: Complete blockade in five mice Tumors grew in three of them. |
| References |
|
| Additional Infomation |
Clospirazine hydrochloride is a member of phenothiazines.
|
| Molecular Formula |
C22H25CL2N3OS2
|
|---|---|
| Molecular Weight |
482.48
|
| Exact Mass |
481.082
|
| CAS # |
27007-85-8
|
| Related CAS # |
Spiclomazine;24527-27-3
|
| PubChem CID |
122820
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.42g/cm3
|
| Boiling Point |
695.3ºC at 760mmHg
|
| Flash Point |
374.3ºC
|
| Vapour Pressure |
3.51E-19mmHg at 25°C
|
| LogP |
6.121
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
601
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.ClC1C=CC2=C(N(C3=CC=CC=C3S2)CCCN2CCC3(SCC(=O)N3)CC2)C=1
|
| InChi Key |
JRSBQVOEILNXGS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H24ClN3OS2.ClH/c23-16-6-7-20-18(14-16)26(17-4-1-2-5-19(17)29-20)11-3-10-25-12-8-22(9-13-25)24-21(27)15-28-22;/h1-2,4-7,14H,3,8-13,15H2,(H,24,27);1H
|
| Chemical Name |
8-[3-(2-chlorophenothiazin-10-yl)propyl]-1-thia-4,8-diazaspiro[4.5]decan-3-one;hydrochloride
|
| Synonyms |
APY606 Spiclomazine Hydrochloride Spiclomazine HCl APY 606 APY-606 Diceplon Disepron Clospirazine 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
|
|---|---|
| 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 | 2.0726 mL | 10.3631 mL | 20.7262 mL | |
| 5 mM | 0.4145 mL | 2.0726 mL | 4.1452 mL | |
| 10 mM | 0.2073 mL | 1.0363 mL | 2.0726 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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