AGN 194310
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 424.55 |
| Cas No. | 229961-45-9 |
| Formula | C28H24O2S |
| Solubility | insoluble in H2O; ≥16.8 mg/mL in DMSO; ≥2.12 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-((4-(4-ethylphenyl)-2,2-dimethyl-2H-thiochromen-6-yl)ethynyl)benzoic acid |
| SDF | Download SDF |
| Canonical SMILES | CCC1=CC=C(C(C2=C(S3)C=CC(C#CC4=CC=C(C(O)=O)C=C4)=C2)=CC3(C)C)C=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
ITS+-grown LNCaP, DU145 and PC3 cells |
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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. |
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Reacting condition |
50 nM, 100 nM, 1 μM |
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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]: | |
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Animal models |
female C57Bl/6J mice |
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Dosage form |
Oral gavage, 0.5 mg/kg/day, 11 days |
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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. |
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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. |
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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. | |
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