Apomine
Based on 1 Customer Validation
Apomine (SR-45023A) is an orally active antineoplastic agent that inhibits the mevalonate/isoprenoid pathway in cholesterol synthesis. Apomine can accelerate the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR). Apomine can also inhibit the growth of various types of cancer cells, including lung cancer, colon cancer, breast cancer, and skin cancer. Apomine is able to induce apoptosis in tumor cell lines derived from leukemia, colon cancer, liver cancer, ovarian cancer, and breast cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.67%
- CAS No.: 126411-13-0
- Formule: C28H52O7P2
- Masse moléculaire:562.66
-
Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
-
HY-100793
SR12813HMG-CoA Reductase Inhibitor/hPXR Agonist -
HY-17504B
Rosuvastatin SodiumHMGCR Inhibitor -
HY-104051
Monacolin JCholesterol Biosynthesis Inhibitor -
HY-114316
HMG499HMGCR Degrader -
HY-129458
CerivastatinHMG-CoA Reductase Inhibitor -
HY-100793R
SR12813 (Standard)HMG-CoA Reductase Inhibitor/hPXR Agonist -
HY-122439
Lovastatin acidHMG-CoA Inhibitor -
HY-17504BR
Rosuvastatin Sodium (Standard)Reference Standard -
HY-17504C
(3R,5R)-RosuvastatinhERG Potassium Channel Blocker/HMG-CoA Reductase Inhibitor
Activité biologique
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.47 μM
Compound: SR45023A
|
Induction of human HMGCR-dCat-ELuc degradation expressed in HEK293 cells assessed as reduction in luciferase activity after 4 hrs by luciferase reporter assay
Induction of human HMGCR-dCat-ELuc degradation expressed in HEK293 cells assessed as reduction in luciferase activity after 4 hrs by luciferase reporter assay
|
[PMID: 31902650] |
In Vitro
Apomine (1-20 μM; 72 h) induces a dose-dependent increase in apoptosis in NCI H929, RPMI 8226 and JJN-3 human myeloma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:NCI H929, RPMI 8226 and JJN-3 human myeloma cells
-
Concentration:2 μM, 10 μM, 15 μM, 20 μM
-
Incubation Time:72 h
-
Result:Induced a dose-dependent increase in apoptosis.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:5T2MM murine myeloma cells were injected into C57BL/KaLwRij mice[2].
-
Dosage:200 mg/kg
-
Administration:Fed for 4 weeks
-
Result:Caused a decrease in serum paraprotein and a decrease in tumor burden. Inhibited the development of osteolytic lesions and prevented the tumor-induced decreases in bone mineral density (BMD).
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 126411-13-0
-
Appearance Solid
-
Masse moléculaire 562.66
-
Formule C28H52O7P2
-
Color Off-white to light yellow
-
SMILES
CC(C)(C)C1=C(O)C(C(C)(C)C)=CC(CC(P(OC(C)C)(OC(C)C)=O)P(OC(C)C)(OC(C)C)=O)=C1
-
Synonyms
SR-45023A; SR 9223i; SK&F-99085
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 20 mg/mL (35.55 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
-
Fiche technique (280 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Kuehl PJ, et al. Preformulation, formulation, and in vivo efficacy of topically applied apomine. Int J Pharm. 2009;382(1-2):104-110. [Content Brief]
[2]. Edwards CM, et al. Apomine, an inhibitor of HMG-CoA-reductase, promotes apoptosis of myeloma cells in vitro and is associated with a modulation of myeloma in vivo. Int J Cancer. 2007 Apr 15;120(8):1657-63. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7773 mL | 8.8864 mL | 17.7727 mL | 44.4318 mL |
| 5 mM | 0.3555 mL | 1.7773 mL | 3.5545 mL | 8.8864 mL | |
| 10 mM | 0.1777 mL | 0.8886 mL | 1.7773 mL | 4.4432 mL | |
| 15 mM | 0.1185 mL | 0.5924 mL | 1.1848 mL | 2.9621 mL | |
| 20 mM | 0.0889 mL | 0.4443 mL | 0.8886 mL | 2.2216 mL | |
| 25 mM | 0.0711 mL | 0.3555 mL | 0.7109 mL | 1.7773 mL | |
| 30 mM | 0.0592 mL | 0.2962 mL | 0.5924 mL | 1.4811 mL |
Apomine Related Classifications
HY-19671 Related Classifications
Powered by Bioz