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| 25mg |
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Purity: ≥98%
AM580 (also named CD336, NSC608001, Ro 40-6055) is a stable retinobenzoic analog that is originally synthesized as a novel, potent and selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively. It is a powerful inducer of granulocytic maturation in NB4, an APL-derived cell line, and in freshly isolated APL blasts. 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. The anticancer effect of RARalpha, together with the newly discovered pro-proliferative role of RARgamma, suggests that specific activation of RARalpha and inhibition of RARgamma might be effective in breast cancer therapy.
| ln Vitro |
In the presence of G-CSF, AM580 (at 10-8 M) significantly increased the expression of LAP mRNA in NB4 cells. When combined with G-CSF, AM580 and ATRA induced almost the same amounts of LAP transcripts at a concentration of 10-5 M. In NB4 cells, AM580 (at 10-8 M) increases steady-state levels of transcripts encoding G-CSF receptors by about six times [1]. In all colonies, AM580 (50 nM) elevates caspase-3 expression, and in 30% of colonies, it causes acinar cavitation [2]. Higher levels of CRBP1 expression were observed following RARη1 knockdown in primary Myc cells using shRARη1 and Am580 treatment, suggesting that RARη has an inhibitory effect on the RARα target gene CRBP1 in these cells. The antiproliferative effects of RARγ knockdown in MCF-10A and MCF-7 cell lines are enhanced by Am580 (200 nM), whereas MDA-MB-231 cells are not affected [3].
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| ln Vivo |
Treatment with am580 (0.3 mg/kg/day) had a more significant impact on the tumor-free survival of MMTV-wnt1 mice; effects were seen in the liver, lung, kidney, and spleen as well as in early-emerging tumors. In both transgenic glands, Am580 treatment significantly and equally decreased the levels of hyperplasia [2]. When administered to MMTV-Myc mice, the RARα selective agonist Am580 can effectively suppress the growth of mammary tumors, lung metastases, and extend tumor latency in 63% of the mice [3].
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| Animal Protocol |
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| References |
[1]. Gianní M, et al. AM580, a stable benzoic derivative of retinoic acid, has powerful and selective cyto-differentiating effects on acute promyelocytic leukemia cells. Blood. 1996 Feb 15;87(4):1520-31.
[2]. Lu Y, et al. Mechanism of inhibition of MMTV-neu and MMTV-wnt1 induced mammary oncogenesis by RARalpha agonist AM580. Oncogene. 2010 Jun 24;29(25):3665-76. [3]. Bosch A, et al. Reversal by RARα agonist Am580 of c-Myc-induced imbalance in RARα/RARγ expression during MMTV-Myc tumorigenesis. Breast Cancer Res. 2012 Aug 24;14(4):R121 |
| Molecular Formula |
C₂₂H₂₅NO₃
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| Molecular Weight |
351.44
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| CAS # |
102121-60-8
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| Related CAS # |
AM580;102121-60-8
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| SMILES |
O=C(O)C1=CC=C(NC(C2=CC=C3C(C)(C)CCC(C)(C)C3=C2)=O)C=C1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 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 (7.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8454 mL | 14.2272 mL | 28.4544 mL | |
| 5 mM | 0.5691 mL | 2.8454 mL | 5.6909 mL | |
| 10 mM | 0.2845 mL | 1.4227 mL | 2.8454 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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