TTNPB (Arotinoid Acid) is a potent RAR agonist, and inhibits binding of [3H]tRA with IC50 of 5.1 nM, 4.5 nM, and 9.3 nM for human RARα, β, and γ, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | T47D cells and 184 cells |
| Preparation method | Human mammary epithelial cells are maintained in Mammary Epithelial Basal Medium (MEBM) supplemented with the Mammary Epithelial Growth Media (MEGM) bullet kit. 184 and 184B5 cells are maintained in MEBM sodium-bicarbonate free (MEBM-SBF) supplemented with the MEGM bullet kit, isoproterenol (10 μM), and transferrin (5 μg/ml). MCF10A cell lines are maintained in DME/F12 containing 5% heat inactivated horse serum, penicillin/streptomycin (100 μg/ml and 100 μg/ml), hydrocortisone (1.4μM), insulin (10 μg/ml), choleratoxin (100 ng/ml), and EGF (20 ng/ml). Breast cancer cell lines are maintained in Improved MEM Zinc Option containing 10% fetal bovine serum, 1% glutamine, and 1% penicillin/streptomycin. For growth assays, cells are treated with the different retinoids for the specified number of days with media and treatment changes every other day in T47D cells and every 2 days in 184 cells. Cell proliferation is measured according to the protocol for the CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay. This colorimetric assay determines the number of viable cells in a sample. Each point represents samples done in quadruplicate |
| Concentrations | ~1 μM |
| Incubation time | 8-12 days |
| Animal Experiment | |
|---|---|
| Animal models | Mouse models bearing hormone-sensitive (HS) and hormone-insensitive (HI) strains of the MXT murine mammary carcinoma. |
| Formulation | Saline |
| Dosages | ~0.25 mg/kg |
| Administration | i.p. |
| Molecular Weight | 348.48 |
| Formula | C24H28O2 |
| CAS Number | 71441-28-6 |
| Solubility (25°C) | DMSO |
| Storage | 2-8°C, protect from light |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related RAR/RXR Products |
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MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist that potently inhibits the expression of iNOS as well as p-ERK protein levels. In addition, MSU-42011 has immunomodulatory and antitumor activities for cancer research. |
| KCL-286
KCL-286 is an orally active retinoic acid receptor-beta (RAR-beta) agonist for studies related to spinal cord injury. |
| XS-060
XS-060 is a potent anticancer agent and RXRα antagonist. |
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| ER 50891 quarterhydrate
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