| 產(chǎn)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 |
| 靶點(diǎn)： |
RAR/RXR;Autophagy;RetinoidReceptor |
| 體外研究： |
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. |
| 體內(nèi)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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京