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• 产品描述： 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

• 靶点： RAR/RXR;Autophagy;RetinoidReceptor

• 体外研究：
  AGN194310 potently inhibits colony formation by all three lines, with IC50 values of 16 nM for LNCaP cells; 18 nM for PC3 cells; and 34 nM for DU-145 cells. AGN 194310 (50 nM, 100 nM; LNCaP, PC-3 and DU-145 cells) inhibits colony formation at concentrations of 50 nM and 100 nM alone and in combination with TTNPB. AGN 194310 (1 μM; 72 hours; LNCaP cells) treatment results in 80% apoptosis. Cell Viability Assay Cell Line: LNCaP, PC-3 and DU-145 cells. Concentration: 50 nM, 100 nM Incubation Time: Result: When used together with 100 nM TTNPB, there was almost complete reversal of the growth inhibitory effect of 50 nM and partial reversal of the effect of 100 nM. Apoptosis Analysis Cell Line: LNCaP cells Concentration: 1 μM Incubation Time: 72 hours Result: Induced apoptosis in LNCaP cells.

• 体内研究：
  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 is 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.

• 参考文献：
  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. 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. 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.355 ml	11.777 ml	23.554 ml
  5 mM	0.471 ml	2.355 ml	4.711 ml
  10 mM	0.236 ml	1.178 ml	2.355 ml
  50 mM	0.047 ml	0.236 ml	0.471 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *