| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Amgen-23 targets sphingosine kinase 1 (SPHK1) and sphingosine kinase 2 (SPHK2), which are enzymes that phosphorylate sphingosine to sphingosine-1-phosphate (S1P). S1P is a bioactive lipid that regulates various cellular processes, including proliferation, survival, and migration. SPHK1 is often overexpressed in cancer, making it a promising therapeutic target. By inhibiting SPHK1 (and to a lesser extent SPHK2), Amgen-23 reduces S1P production, thereby inhibiting cancer cell growth and survival.
|
|---|---|
| ln Vitro |
In vitro, Amgen-23 is a potent inhibitor of SPHK1 with an IC50 of 20 nM and inhibits SPHK2 with an IC50 of 1.6 μM. This demonstrates its high potency and selectivity for SPHK1 over SPHK2. Its activity is characterized in kinase inhibition assays measuring the phosphorylation of sphingosine.
|
| ln Vivo |
Specific in vivo activity data for Amgen-23 are not provided in the available sources. As a potent SPHK1 inhibitor, it would be expected to have antitumor activity in animal models. However, no specific studies are described.
|
| Enzyme Assay |
A cell-free assay for Amgen-23 involves measuring its inhibition of SPHK1 and SPHK2 kinase activity. Recombinant SPHK1 or SPHK2 is incubated with sphingosine and ATP in the presence of varying concentrations of the compound. The production of S1P is measured, and the IC50 is calculated. For Amgen-23, the IC50 values are 20 nM for SPHK1 and 1.6 μM for SPHK2.
|
| Cell Assay |
Cellular assays for Amgen-23 would typically involve assessing its effects on S1P production and cancer cell viability. Cells are treated with the compound, and the levels of S1P are measured by mass spectrometry. Cell proliferation and apoptosis assays are used to assess the compound's functional effects.
|
| Animal Protocol |
In vivo animal experiments for Amgen-23 are not described in the available sources. As a research compound with anticancer potential, it could be evaluated in tumor xenograft models. However, no specific protocols or data are provided.
|
| ADME/Pharmacokinetics |
Amgen-23 has a molecular formula of C23H25Cl2N3O2S and a molecular weight of 478.4 g/mol. Specific pharmacokinetic parameters are not provided in the available sources. As a research compound, it is intended for preclinical studies.
|
| Toxicity/Toxicokinetics |
Toxicity data for Amgen-23 are not provided in the available sources. As a research compound, it is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be observed.
|
| References | |
| Additional Infomation |
Amgen-23 (CAS: 1448706-15-7) is a potent inhibitor of sphingosine kinase 1 (SPHK1) with an IC50 of 20 nM. It also inhibits SPHK2 with an IC50 of 1.6 μM. The compound is used in anticancer research. It is not an approved drug and is strictly for research purposes.
|
| Molecular Formula |
C23H25CL2N3O2S
|
|---|---|
| Molecular Weight |
478.43
|
| Exact Mass |
477.104
|
| CAS # |
1448706-15-7
|
| PubChem CID |
71627420
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.3
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
31
|
| Complexity |
555
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
N1(CCC2=CC=C(NC3=NC(C4=CC=C(Cl)C(Cl)=C4)=CS3)C=C2)CC[C@H](O)C[C@@H]1CO
|
| InChi Key |
SQJKFWCRPARYPY-MOPGFXCFSA-N
|
| InChi Code |
InChI=1S/C23H25Cl2N3O2S/c24-20-6-3-16(11-21(20)25)22-14-31-23(27-22)26-17-4-1-15(2-5-17)7-9-28-10-8-19(30)12-18(28)13-29/h1-6,11,14,18-19,29-30H,7-10,12-13H2,(H,26,27)/t18-,19+/m1/s1
|
| Chemical Name |
(2R,4S)-1-[2-[4-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]amino]phenyl]ethyl]-2-(hydroxymethyl)piperidin-4-ol
|
| 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) |
DMSO : ~100 mg/mL (~209.02 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.23 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 25.0 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: 2.5 mg/mL (5.23 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (5.23 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 | 2.0902 mL | 10.4508 mL | 20.9017 mL | |
| 5 mM | 0.4180 mL | 2.0902 mL | 4.1803 mL | |
| 10 mM | 0.2090 mL | 1.0451 mL | 2.0902 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
