| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
Akt
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|---|---|
| ln Vitro |
K-80003 inhibits TNF-induced colocalization of tRXRα with p85α in the cytoplasm, leading to tRXRα nuclear localization, in MCF-7 cells. Western blotting demonstrates that the tRXRα monomer is distributed in both the nuclear and cytoplasmic fractions while the K-80003-stabilized tetrameric form of tRXRα is only found in the nuclear fraction[2].
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| ln Vivo |
K-80003 is a potent inhibitor of AKT activation by all-trans-retinoic acid. Inhibiting tRXRα-dependent AKT activation and tRXRα tumor growth in animals with K-80003 shows improved efficacy. Despite lacking COX inhibitory activity, K-80003 has a high affinity for RXRα[1].
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| Cell Assay |
K-80003 (5 μM) is pretreated with or without for 3 hours before TNF (10 ng/mL) is applied to MCF-7 cells that have been cotransfected with Myc-RXRα, Myc-tRXRα, tRXRα/L433D and p85α.
Anti-Myc and anti-p85α antibodies are used to stain the cells, and confocal microscopy is used to determine where in the cell they are located. K-80003 (5 μM) is administered to or left untreated for 6 hours to HEK293T cells that have been cotransfected with Myc-tRXRα . By using an anti-Myc antibody and western blotting to analyze the nuclear (N) and cytoplasmic (C) fractions after BS3 crosslinking. Examining the expression of cytoplasmic -tubulin and nuclear PARP in non-crosslinked fractions allows one to determine the purity of the fractions. The first of three related experiments is displayed[2].
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| Animal Protocol |
Mice[1]: Subcutaneous injection of 100 L of cells (2106) is performed on naked mice (BALB/c, 4-5 weeks old). Mice (n=6) are given intraperitoneal injections of K-80003, Sulindac, or corn oil once every other day (total of six injections) for a period of seven days following transplantation. Every 4 days, measurements are made of the body weight and tumor sizes.
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| References |
| Molecular Formula |
C22H21FO2
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|---|---|
| Molecular Weight |
336.399349927902
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| Exact Mass |
336.1526
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| Elemental Analysis |
C, 78.55; H, 6.29; F, 5.65; O, 9.51
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| CAS # |
1292821-90-9
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| Related CAS # |
1292821-90-9
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| Appearance |
Solid powder
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| SMILES |
O=C(O)CC(C1=C/2C=CC(F)=C1)=C(C)C2=C\C3=CC=C(C(C)C)C=C3
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| InChi Key |
QCXBVGNDRYQVJO-GRSHGNNSSA-N
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| InChi Code |
InChI=1S/C22H21FO2/c1-13(2)16-6-4-15(5-7-16)10-19-14(3)20(12-22(24)25)21-11-17(23)8-9-18(19)21/h4-11,13H,12H2,1-3H3,(H,24,25)/b19-10-
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| Chemical Name |
1H-Indene-3-acetic acid, 5-fluoro-2-methyl-1-((4-(1-methylethyl)phenyl)methylene)-, (1Z)-
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| Synonyms |
K 80003; K-80003; K80003
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~30 mg/mL (89.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (8.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 30.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9727 mL | 14.8633 mL | 29.7265 mL | |
| 5 mM | 0.5945 mL | 2.9727 mL | 5.9453 mL | |
| 10 mM | 0.2973 mL | 1.4863 mL | 2.9727 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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