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AGN 194310

In stock
Catalog No.
B4702
pan-RAR antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$780.00
In stock
1mg
$300.00
In stock

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Background

AGN 194310 is a pan-antagonist of retinoic acid receptors (RARs) with Kd values of 3nM, 2nM and 5nM for RAR α, RARβ and RARγ, respectively [1].

AGN 194310 has been reported to bind to RARs with equal and high Kd values of 3, 2 and 5nM for RAR α, RARβ and RARγ, respectively, by in vitro binding experiments. In addition, AGN 194310 has been revealed to potently inhibit the colony formation by ITS+-grown cell lines with IC50 values of 16 ± 5nM for LNCaP cells; 18 ± 6nM for PC3 cells; and 34 ± 7nM for DU-145 cells. Apart from these, because of binding to and mediating the effects via RARs, AGN 194310 has been demonstrated to inhibit agonist-induced (TTNPB) differentiation of HL60 cells. AGN 194310 has also shown the accumulation of cell in G1 and the function of induced apoptosis [1].

References:
[1] Hammond LA1, Van Krinks CH, Durham J, Tomkins SE, Burnett RD, Jones EL, Chandraratna RA, Brown G. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells.Br J Cancer. 2001 Aug 3; 85(3):453-62.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt424.55
Cas No.229961-45-9
FormulaC28H24O2S
Solubility≥16.8mg/mL in DMSO
Chemical Name4-((4-(4-ethylphenyl)-2,2-dimethyl-2H-thiochromen-6-yl)ethynyl)benzoic acid
SDFDownload SDF
Canonical SMILESCCC1=CC=C(C(C2=C(S3)C=CC(C#CC4=CC=C(C(O)=O)C=C4)=C2)=CC3(C)C)C=C1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

ITS+-grown LNCaP, DU145 and PC3 cells

Preparation method

The solubility of this compound in DMSO is > 16.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

50 nM, 100 nM, 1 μM

Applications

In ITS+-grown LNCaP, DU145 and PC3 cells, AGN194310 (50 nM and 100 nM) potently inhibited colony formation. AGN194310 (1 μM) caused cells to accumulate in G1 and undergwent apoptosis. In primary prostate carcinoma cells, AGN194310 (10 and 100 nM) caused substantial growth inhibition.

Animal experiment [2]:

Animal models

female C57Bl/6J mice

Dosage form

Oral gavage, 0.5 mg/kg/day, 11 days

Application

Treatment with AGN194310 significantly increased the number and proportion of granulocytes. Treatment with AGN194310 significantly increased the frequency of progenitor cells containing granulocytes in the bone marrow of mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Hammond L A, Van Krinks C H, Durham J, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells[J]. British journal of cancer, 2001, 85(3): 453.

[2]. Walkley C R, Yuan Y D, Chandraratna R A S, et al. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis[J]. Leukemia, 2002, 16(9): 1763.

Quality Control

Quality Control & MSDS

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Chemical structure

AGN 194310

Related Biological Data

AGN 194310