AGN 194310
Names
[ CAS No. ]:
229961-45-9
[ Name ]:
AGN 194310
[Synonym ]:
4-{[4-(4-Ethylphenyl)-2,2-dimethyl-2H-thiochromen-6-yl]ethynyl}benzoic acid
Benzoic acid, 4-[2-[4-(4-ethylphenyl)-2,2-dimethyl-2H-1-benzothiopyran-6-yl]ethynyl]-
Biological Activity
[Description]:
AGN 194310(VTP-194310) is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM for RARα/β/γ respectively.IC50 value: 3/2/5 nM (Kd for RARα/β/γ) [1][2]Target: RARs agonistin vitro: A high affinity pan-RAR antagonist (AGN194310, K(d) for binding to RARs = 2-5 nM) inhibited colony formation (by 50%) by all three lines at 16-34 nM, and led to a transient accumulation of flask-cultured cells in G1 followed by apoptosis. AGN194310 is 12-22 fold more potent than all-trans retinoic acid (ATRA) against cell lines and also more potent in inhibiting the growth of primary prostate carcinoma cells [2].in vivo: The administration of all-trans retinoic acid to VAD mice resulted in a transient reduction in NF-kappaB activity and, conversely, a single dose of the RAR-pan-antagonist, AGN 194310, administered to control mice, led to a marked, transient induction of whole-body luminescence [3]. Mice were treated with AGN194310, a synthetic retinoid that antagonises the physiological function of the three RAR isotypes (alpha, beta, gamma) but does not interact with RXRs. Analyses of the granulocytic lineage using Gr-1, c-Kit and CD11b antibodies, demonstrated that granulocyte numbers were strikingly increased across haemopoietic compartments in all AGN194310-treated mice. A significant increase in the frequency of progenitor cells containing granulocytes was observed in the bone marrow of mice following treatment with AGN194310 [4].
[Related Catalog]:
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Density]:
1.3±0.1 g/cm3
[ Boiling Point ]:
598.1±50.0 °C at 760 mmHg
[ Molecular Formula ]:
C28H24O2S
[ Molecular Weight ]:
424.554
[ Flash Point ]:
315.5±30.1 °C
[ Exact Mass ]:
424.149689
[ LogP ]:
9.56
[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C
[ Index of Refraction ]:
1.683
[ Storage condition ]:
2-8℃