ARV-825

製品コードS8297

ARV-825化学構造

分子量(MW):923.43

ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.

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文献中Selleckの製品使用例(1)

製品安全説明書

Epigenetic Reader Domain阻害剤の選択性比較

生物活性

製品説明 ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.
ターゲット
BRD4 BD2 [1]
(Cell-free assay)
BRD4 BD1 [1]
(Cell-free assay)
28 nM(Kd) 90 nM(Kd)
体外試験

Compared with the BRD4 inhibitors, ARV-825 treatment results in a strikingly more pronounced effect on the levels of c-MYC, and downstream cell proliferation and apoptosis induction in BL (Burkitt’s Lymphoma) cell lines[1]. The IC50s of ARV-825 for all tested cell lines and primary AML cells at 72 hours are in the low nanomolar range (2-50 nM). ARV-825 treatment reduces PIM1 levels and phosphorylation of CXCR4 in AML cells while overexpression of PIM1 or Myc reverses the phenomena[3].

アッセイ
Methods Test Index PMID
Western blot
BRD1 / BRD2 / BRD3 / BRD4 / p21; 

PubMed: 30903020     


Temporal effects of ARV-825 and OTX015 (200 nM) on indicated proteins in LPS141 cells. 

c-MYC; 

PubMed: 26051217     


Namalwa (left) and Ramos (right) cells were treated overnight with increasing doses of ARV-825 (up to 1.0 µM), or JQ1 (up to 10.0 µM), or OTX015 (up to 10.0 µM); lysates were analyzed by immunoblot for BRD4, c-MYC and actin.

PARP / cleaved PARP ; 

PubMed: 26051217     


Ramos and CA-46 cells were treated with increasing doses of ARV-825 (up to 1.0 µM), or JQ1 and OTX015 (up to 10.0 µM) for 48 hours. Lysates were collected and analyzed by immunoblot for PARP cleavage with actin as loading control

CDK6 / CDK4 ; 

PubMed: 29581547     


Effects of ARV-825 and ARV-763 on the expression levels of p21, CDK4, and CDK6 were examined by Western blotting of MM1.S cell extracts 24 hours after exposure to the indicated drug concentrations of drugs, with β-actin used as a loading control.

cleaved caspase 9 / cleaved caspase 3 ; 

PubMed: 29581547     


Programmed cell death activation was confirmed by preparing lysates of the indicated myeloma cell lines and subjecting them to Western blotting for cleaved PARP, Caspase-3 and -9, and β-actin as a loading control.

Akt / pAKT-S473 / mTOR / p-mTOR-S2448 / p70S6K / p70S6K-T389 / 4EBP1/ p-4EBP1-S65 / PDK1 / p-PDK1-S241 / PI3K / p-PI3K-T458; 

PubMed: 29581547     


The effect of ARV-825 or ARV-763 on the expression levels of key intermediates in the PI3K-Akt-mTOR pathway signaling were probed by Western blotting of MM1.S (left panel) and RPMI 8226 (right panel) cells. These were exposed for 24 hours to the indicated䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð

JAK2 / p-STAT5 / p-STAT3 / PIM1 / p27 / Bcl-xl / γH2AX; 

PubMed: 28042144     


SET-2 cells were treated with the indicated concentrations of ARV-825 or OTX015 for 18 hours. Total cell lysates were prepared and immunoblot analyses were conducted as indicated. The expression levels of β-Actin in the cell lysates served as the loading 䲧疝Ỵ疞

30903020 26051217 29581547 28042144
Immunofluorescence
BRD4 ; 

PubMed: 28042144     


SET2 cells were treated with the indicated concentrations of ARV-825 or OTX015 for 16 hours. Then, cells were cytospun onto glass slides and immunostained for BRD4 expression. Cells were counterstained with DAPI and images were acquired utilizing confocal䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖

28042144
Growth inhibition assay
Cell viability ; 

PubMed: 26051217     


Various BL cell lines were seeded at 50000 cells/100ul in 96-well plates and then treated with increasing doses of ARV-825, JQ1 and OTX015; relative proliferation was determined by CellTiter-Glow (CTG) assay 72 hours later.

26051217
体内試験

In a mouse model of human leukemia, the leukemia burdens are significantly lower in the ARV-825 treated mice as confirmed by luciferase imaging, flow cytometry, spleen size and survived longer compared to control mice[3].

お薦めの試験操作(参考用のみ)

細胞試験:

[2]

- 合併
  • 細胞株: RS4;11 cells
  • 濃度: 3, 10, 30 nM
  • 反応時間: 3 h
  • 実験の流れ:

    RS4;11 cells are treated for 3 h with each individual compound at indicated concentrations, and proteins are probed by specific antibodies.


    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (108.29 mM)
Ethanol 3 mg/mL (3.24 mM)
Water Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 923.43
化学式

C46H47ClN8O9S

CAS No. 1818885-28-7
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

Epigenetic Reader Domainシグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID