| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
SphK1
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|---|---|
| ln Vitro |
In HCT116 cells and HCT116 cells expressing TP53 null tumors, SK1-I hydrochloride (0-10 μM; 24 hours) attenuates cancer cell proliferation and survival in a TP53-dependent manner[2]. Compared to HCT116 cells without TP53, SK1-I hydrochloride (0–20 μM; 12 hours) causes more CASP3 cleavage in HCT116 cells, resulting in a characteristic of apoptosis[2].
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| ln Vivo |
The hypotensive response is greatly reduced when SK1-I hydrochloride (BML-258 hydrochloride; intraperitoneal (ip) injection; once; 24 hours previous to baseline mean arterial blood pressure (MAP); 75 mg/kg) is administered before anandamide (iv injection; two doses; 1 and 10 mg/kg)[3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: HCT116 cells and HCT116 cells bearing TP53 null cancer Tested Concentrations: 0 µM, 2.5 µM, 5 µM, 7.5 µM, 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished cancer cell growth and survival. Western Blot Analysis[2] Cell Types: HCT116 cells and HCT116 cells bearing TP53 null cancer Tested Concentrations: 0 µM, 5 µM , 10 µM, 20 µM Incubation Duration: 12 hrs (hours) Experimental Results: Induced more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (24 ± 3.5 g)[3]
Doses: 75 mg/kg Route of Administration: intraperitoneal (ip) injection; once; 24 hrs (hours) prior to baseline MAP measurement Experimental Results: Dramatically lowered baseline mean arterial blood pressure (MAP). |
| References |
[1]. Melissa R Pitman, et al. Inhibitors of the sphingosine kinase pathway as potential therapeutics. Curr Cancer Drug Targets. 2010 Jun;10(4):354-67.
[2]. Santiago Lima, et al. TP53 is required for BECN1- and ATG5-dependent cell death induced by sphingosine kinase 1 inhibition. Autophagy. 2018;14(6):942-957. [3]. Fiona H Greig, et al. Requirement for sphingosine kinase 1 in mediating phase 1 of the hypotensive response to anandamide in the anaesthetised mouse. Eur J Pharmacol. 2019 Jan 5;842:1-9. |
| Molecular Formula |
C17H28CLNO2
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|---|---|
| Molecular Weight |
313.86
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| CAS # |
2366222-05-9
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| Related CAS # |
SK1-I;1072443-89-0
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| SMILES |
Cl.C(/C1C=CC(CCCCC)=CC=1)=C\[C@H](O)[C@H](NC)CO
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (796.53 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.63 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 20.8 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: ≥ 2.08 mg/mL (6.63 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 20.8 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: ≥ 2.08 mg/mL (6.63 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 | 3.1861 mL | 15.9307 mL | 31.8613 mL | |
| 5 mM | 0.6372 mL | 3.1861 mL | 6.3723 mL | |
| 10 mM | 0.3186 mL | 1.5931 mL | 3.1861 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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