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AM580

Cat. No. M7568
AM580 Structure
Synonym:

CD336; NSC608001; Ro 40-6055

Size Price Availability Quantity
5mg USD 62  USD62 In stock
10mg USD 88  USD88 In stock
50mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Huebner H, et al. J Exp Clin Cancer Res. Hypermethylation and loss of retinoic acid receptor responder 1 expression in human choriocarcinoma.

[2] Perri M, et al. Exp Cell Res. BCL-xL/MCL-1 inhibition and RARγ antagonism work cooperatively in human HL60 leukemia cells.

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Keywords: AM580, CD336; NSC608001; Ro 40-6055 supplier, RAR/RXR, inhibitors, activators


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