| Identification | Back Directory | [Name]
AGN 194310 | [CAS]
229961-45-9 | [Synonyms]
AGN
CS-1211
VTP194310
VTP-194310
AGN 194310
VTP 194310
AGN-194310, 194310
AGN194310; AGN-194310; VTP194310; VTP 194310; VTP-194310
Benzoic acid, 4-[2-[4-(4-ethylphenyl)-2,2-dimethyl-2H-1-benzothiopyran-6-yl]ethynyl]- | [Molecular Formula]
C28H24O2S | [MOL File]
229961-45-9.mol | [Molecular Weight]
424.55 |
| Chemical Properties | Back Directory | [Boiling point ]
598.1±50.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
>16.8mg/mL in DMSO | [form ]
Powder | [pka]
4.02±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively[1][2]. AGN 194310 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [Biological Activity]
AGN 194310 (VTP-194310) is a high-affinity, potent, and selective pan-antagonist of retinoic acid receptors (RARs) with Kd values of 3 nM and 2 nM for RARα, RARβ, and RARγ, respectively , 5 nM. | [in vivo]
AGN 194310 (0.5 mg/kg/day; oral gavage; every day; for 10 days; female C57Bl/6J mice) treatment increases the number of granulocytes across haemopoietic compartments. A significant increase in the frequency of granulocyte -progenitor cells are observed in the bone marrow of mice after treatment with AGN194310. | Animal Model: | Female C57Bl/6J mice (Five -week-old (34-37 days)) | | Dosage: | 0.5 mg/kg/ day | | Administration: | Oral gavage; every day; for 10 days | | Result: | The number of granulocytes was significantly increased across haemopoietic compartments. Progenitor cells containing granulocytes also increased significantly. | | [target]
| RARα 3 nM (Kd) | RARβ 2 nM (Kd) | RARγ 5 nM (Kd) | < /table>[storage]
Store at -20°C | [References]
[1] Johnson AT, et al. Synthesis and biological activity of high-affinity retinoic acid receptor antagonists. Bioorg Med Chem. 1999 Jul;7(7):1321-38. DOI:10.1016/s0968-0896(99)00055-3
[2] Hammond LA, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells. Br J Cancer. 2001 Aug 3;85(3):453-62. DOI:10.1054/bjoc.2001.1939
[3] Walkley CR, et al. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis. Leukemia. 2002 Sep;16(9):1763-72. DOI:10.1038/sj.leu.2402625 |
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BOC Sciences
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SPIRO PHARMA
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www.spiropharma.com.cn |
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Musechem
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+1-800-259-7612 |
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Cckinase, Inc.
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www.cckinase.com |
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Tags:229961-45-9
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