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AR-42
AR-42
AR-42
商品货号:CL-10478
CAS 号:935881-37-1
英文名字:AR-42
质量标准:>98%,HDAC抑制剂
分子式:C18H20N2O3
  • 包装规格:
    规格 库存 发货时间
    2mg [¥900.00]15 现货,一周内发货
    5mg [¥1930.00]15 现货,一周内发货
    10mg [¥3480.00]15 现货,一周内发货
    50mg [¥12510.00]15 现货,一周内发货
  • 购买数量:
  • 会员尊享价:

    商品信息

    质检证书(coa)

    说明书下载

     AR42

    分子式C18H20N2O3    分子量C18H20N2O3

     

    产品描述

    AR-42 (OSU-HDAC42)HDAC抑制剂,IC5030 nM

    靶点

    HDAC

             

    IC50

    30 nM

             

    体外研究

    AR-42 treatment induces histone hyperacetylation and p21WAF/CIP1 overexpression, and inhibits the growth of DU-145 cells with IC50 of 0.11 μM.HDAC42 is potent in suppressing the proliferation of U87MG and PC-3 cells, in part, because of its ability to down-regulate Akt signaling.AR-42 inhibits the growth of PC-3 and LNCaP cells with IC50 of 0.48 μM and 0.3 μM, respectively. Compared to SAHA, AR-42 exhibits distinctly superior apoptogenic potency, and causes markedly greater decreases in phospho-Akt, Bcl-xL, and survivin in PC-3 cells.AR-42 treatment induces growth inhibition, cell- cycle arrest, apoptosis, and activation of caspases-3/7 in malignant mast cell lines. AR-42 treatment induces down-regulation of Kit via inhibition of Kit transcription, disassociation between Kit and heat shock protein 90 (HSP90), and up-regulation of HSP70. AR-42 treatment down-regulates the expression of p-Akt, total Akt, phosphorylated STAT3/5 (pSTAT3/5), and total STAT3/5.AR-42 potently inhibits the growth of JeKo-1, Raji, and 697 cells with IC50 of <0.61 μM. AR-42 also sensitizes CLL cells to TNF-Related Apoptosis Inducing Ligand (TRAIL), potentially through reduction of c-FLIP.AR-42 treatment also induces autophagy through downregulation of Akt/mTOR signaling and inducing ER stress in hepatocellular carcinoma (HCC) cells.

    体内研究

    The growth of PC-3 tumor xenografts is suppressed by 52% and 67% after treatment with AR-42 at 25 mg/kg and 50 mg/kg, respectively, whereas SAHA at 50 mg/kg suppresses growth by 31%. In contrast to mice treated with SAHA, intratumoral levels of phospho-Akt and Bcl-xL are markedly reduced in AR-42 treated mice.In the transgenic adenocarcinoma of the mouse prostate (TRAMP) model, administration of AR-42 not only decreases the severity of prostatic intraepithelial neoplasia (PIN) and completely prevents its progression to poorly differentiated carcinoma, but also shifts tumorigenesis to a more differentiated phenotype, suppressing absolute and relative urogenital tract weights by 86% and 85%, respectively.AR-42 significantly reduces leukocyte counts, and prolongs survival in three separate mouse models of B-cell malignancy without evidence of toxicity.

    溶解性

    DMSO 63 mg/mL,水 <1 mg/mL,乙醇 63 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

    More potent than SAHA.

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