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In vitro: In the presence of G-CSF, AM580 (at 10-8 M) produces a remarkable induction in LAP mRNA of NB4 cells. At a concentration of 10-5 M, AM580 and ATRA, in combination with G-CSF, induce almost the same level of LAP transcript. AM580 (at 10-8 M) leads to an approximately sixfold increase in the steady-state levels of the transcript coding for the G-CSF receptor in NB4 cells. AM580 (50 nM) increases caspase-3 expression in all of the colonies, and in 30% of the colonies induce acinar-like cavitation. Knockdown of RARγ1 in primary Myc cells using shRARγ1 followed by Am580 treatment results in an even higher level of CRBP1 expression, showing that in these cells RARγ has a repressive effect on the RARα target gene CRBP1. Am580 (200 nM) enhances the anti-proliferative effect exhibited by RARγ knockdown in the MCF-10A and MCF-7 cell lines but not in the MDA-MB-231 cells.
In vivo: Am580 (0.3 mg/kg/day) treatment has a more profound effect on tumor-free survival of MMTV-wnt1 mice, the effect being noticeable even in early appearing tumors, and no overt toxicity is found in liver, lungs, kidney, and spleen. Am580 treatment reduces substantially and equally the level of hyperplasia in both transgenic glands. Treatment of MMTV-Myc mice with the RARα-selective agonist Am580 leads to significant inhibition of mammary tumor growth, lung metastasis and extends tumor latency in 63% of mice.
Developmental Biology. 2024 Jun 21;16(1):2347722.
ATRA regulates myoblast differentiation and fusion through the RARα/Pitx2 signaling pathway, causing abnormal development of PFMs in ARM fetal rats.
AM580 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | Leukemic cells |
| Preparation method | Leukemic cells were incubated with various concentrations of JY-1-106 (2–20 μM) alone or with DMSO (as a vehicle) at different time point in 96-well plates. Cells treated with SR11253 200 nM, Am580 200 nM and RA 1 μM individually or together with JY-1-106 (12 μM) for 48 h. |
| Concentrations | 200 nM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 351.44 |
| Formula | C22H25NO3 |
| CAS Number | 102121-60-8 |
| Solubility (25°C) | 45 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related RAR/RXR Products |
|---|
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Acitretin (Ro 10-1670) is a second-generation retinoid. |
| Adapalene
Adapalene is a third-generation topical retinoid, it is a potent RAR agonist, with AC50 values of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene is also an MST1 agonist. |
| Tamibarotene
Tamibarotene is a synthetic retinoic acid receptor (RAR) agonist with high specificity for RARα and RARβ over RARγ. |
| TTNPB
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. |
| Fenretinide
Fenretinide (4-HPR) is a synthetic retinoid deriverative. Fenretinide is shown to exhibit binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death. |
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