JNJ-7706621

製品コードS1249

JNJ-7706621化学構造

分子量(MW):394.36

JNJ-7706621は一種のパン-CDK阻害剤です。NJ-7706621はCDK1/2を抑制する作用が一番強くて、無細胞試験でIC50値が9 nM/4 nMになりますが、CDK1/2に作用する選択性はCDK3/4/6に作用する選択性より6倍以上がそれぞれ高くなって、オーロラA/Bにも有効に抑制することができますが、Plk1とWee1に抑制活性を表しません。

サイズ 価格(税別) 在庫  
JPY 39010.00 あり
JPY 19920.00 あり
JPY 34860.00 あり
JPY 61420.00 あり
JPY 144420.00 あり

カスタマーフィードバック(5)

  • JNJ-7706621 treatment of tamoxifen-resistant cell lines leads to arrest in the G2 cell cycle phase. M phase cells from the upper right quadrants were quantified relative to total G2/M phase cells. Statistical significant differences from vehicle-treated cells are denoted by asterisks; *P<0.05, **P<0.01.

    Oncogene 2014 10.1038/onc.2014.351. JNJ-7706621 purchased from Selleck.

    J558 cells were treated with RO3306 (5-15 umol/L), or JNJ7706621 (0.2-4 umol/L) for 6 hours, after which Western blot analysis was performed to monitor XBP-1s expression.

    Mol Cancer Ther 2014 13(3), 662-74. JNJ-7706621 purchased from Selleck.

  • C) CDK1 activity is inhibited by phosphorylation of Thr14/Tyr15 residues. Dephosphorylation of these residues activates CDK1 and promotes GVBD. In Flavopiridol-treated oocytes, the level of pCDK1 did not change compared with the control group, but Dinaciclib, and less potently JNJ, elevated the level of inhibitory phosphorylation of CDK1. In all groups, the level of pCDK1 was normalized with pan CDK1.

    PLoS One, 2016, 11(3):e0152254. JNJ-7706621 purchased from Selleck.

    Western blot analysis of p-histone , histone, Aurora A and p-Aurora A/B/C. 0-10μM JNJ-7706621 was added.

     

     

    Dr. Zhang of Tianjin Medical University. JNJ-7706621 purchased from Selleck.

  • For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of JNJ-7706621 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.

    Dr. Yong-Weon Yi from Georgetown University Medical Center. JNJ-7706621 purchased from Selleck.

製品安全説明書

CDK阻害剤の選択性比較

生物活性

製品説明 JNJ-7706621は一種のパン-CDK阻害剤です。NJ-7706621はCDK1/2を抑制する作用が一番強くて、無細胞試験でIC50値が9 nM/4 nMになりますが、CDK1/2に作用する選択性はCDK3/4/6に作用する選択性より6倍以上がそれぞれ高くなって、オーロラA/Bにも有効に抑制することができますが、Plk1とWee1に抑制活性を表しません。
特性 A broad-spectrum inhibitor.
ターゲット
CDK2/CyclinE [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
Aurora A [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
3 nM 4 nM 9 nM 11 nM 15 nM
体外試験

JNJ-7706621 also shows some inhibition to VEGF-R2, FGF-R2, and GSK3β, with IC50 of 154-254 nM. JNJ-7706621 shows inhibitory effect on a panel of human cancer cell types, including HeLa, HCT-116, SK-OV-3, PC3, DU145, A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with IC50 of 112-514 nM, independent of p53, retinoblastoma, or P-glycoprotein status. JNJ-7706621 is several-fold less potent at inhibiting growth of normal cell types, including MRC-5, HASMC, HUVEC, and HMVEC, with IC50 of 3.67-5.42 μM. In HeLa or U937 cells, JNJ-7706621 (0.5-3 μM) delays exit from G1, arrests cells in G2-M, induces endoreduplication, activates apoptosis, and reduces colony formation. [1] In a HeLa cell line, incremental treatment with increasing concentrations of JNJ-7706621 leads to a 16-fold resistance, which may be mediated by ABCG2. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 cells MX3GeY5kfGmxbjDhd5NigQ>? NXO2e|RKUW5idnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGi3bXHuJHBENTNiKIDyc5N1[XSnIHHk[Y5w[2G{Y3nuc41iMSC2dX3vdkBk\WyuczygTWM2OD1yLkGyJO69VQ>? MVWxOVk4PDV5MR?=
HCT116 cells NInFV2JHfW6ldHnvckBie3OjeR?= NEf5NlJKdiC4aYTyc{BqdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDj[YxtKHC{b3zp[oVz[XSrb36gbY4hcHWvYX6gTGNVOTF4IDjjc4xwdiClYYLjbY5wdWFrIIT1cY9zKGOnbHzzMEBKSzVyPUCuNlUh|ryP M{nrUFE2QTd2NUex
human HeLa cells MkLVSpVv[3Srb36gZZN{[Xl? Mn3RTY4hfmm2cn:gbY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiY3XscEBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIFjlUIEhMGOnco\pZ4FtKGGmZX7vZ4Fz[2mwb33hLUB1fW2xcjDj[YxteyxiSVO1NF0xNjJ6IN88US=> NW\qdY9JOTV7N{S1O|E>
human A375 cells MoDPVJJwdGmoZYLheIlwdiCjc4PhfS=> NIDSVGhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOsJGlEPTB;MD60OFch|ryP NXTCeIpvOTZ4OEKxPFY>
MDA-MB-231 cells MnSzSpVv[3Srb36gZZN{[Xl? NGjqc5RKdiC4aYTyc{BqdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDj[YxtKHC{b3zp[oVz[XSrb36gbY4hfmG{aX;1d{BpfW2jbjDNSGEuVUJvMkOxJEhjemWjc4SgZ4Fz[2mwb33hLUB1fW2xcjDj[YxteyxiSVO1NF0xNjV7IN88US=> MnLMNVU6PzR3N{G=
SK-OV-3 cells NYC4NGw3TnWwY4Tpc44h[XO|YYm= MkC0TY4hfmm2cn:gbY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiY3XscEBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIGPLMW9XNTNiKH;2ZZJq[W5iYXTlco9k[XKlaX7vcYEqKHS3bX;yJINmdGy|LDDJR|UxRTBwN{Wg{txO NXLYWWxFOTV7N{S1O|E>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 In mouse xenograft model of A375 melanoma human tumor, JNJ-7706621 (100 or 125 mg/kg) causes tumor regression. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

In vitro kinase assay for CDK1 and Aurora kinases:

For CDK1 kinase activity, a method is developed using the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a reduced amount of 33P-γ-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO 4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 and incubated at 30 °C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. Linear regression analysis of the percent inhibition by JNJ-7706621 is used to determine IC50. The Aurora kinase assays are done with 10 μM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif.
細胞試験: [3]
+ 展開
  • 細胞株: HeLa, HCT-116, A375, SK-OV-3, MDA-MB-231, and PC-3 cells
  • 濃度: 1 nM - 10 μM, dissolved in DMSO
  • 反応時間: 48 hours
  • 実験の流れ: The ability of JNJ-7706621 to inhibit the proliferation of cell growth is determined by measuring incorporation of 14C-labelled thymidine into newly synthesized DNA within the cells. Cells are trypsinized and counted and 3-8 × 103 cells are added to each well of a 96-well CytoStar tissue culture treated scintillating microplate in complete medium in a volume of 100 μL. Cells are incubated for 24 hours in complete medium at 37 °C in an atmosphere containing 5% CO2. Next, 1 μL of JNJ-7706621 is added to the wells of the plate. Cells are incubated for 24 more hours. Methyl 14C-thymidine 56 mCi/mmol is diluted in complete medium and 0.2 μCi/well is added to each well of the CytoStar plate in a volume of 20 μL. The plate is incubated for 24 hours at 37 °C in JNJ-7706621 plus 14C-thymidine. The contents of the plate are discarded and the plate is washed twice with 200 μL PBS. 200 μL of PBS is added to each well. The top of the plate is sealed with a transparent plate sealer and a white plate backing sealer is applied to the bottom of the plate. The degree of methyl 14C-thymidine incorporation is quantified on a Packard Top Count.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: Mouse xenograft model of A375 cells
  • 製剤: Dissolved in 0.5% methylcellulose containing 0.1% polysorbate 80 in sterile water.
  • 投薬量: 100 or 125 mg/kg
  • 投与方法: Orally or by intraperitoneal injection injection
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 79 mg/mL (200.32 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
0.5% methylcellulose+0.2% Tween 80
14 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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 394.36
化学式

C15H12F2N6O3S

CAS No. 443797-96-4
保管
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

CDK信号経路図

CDK Inhibitors with Unique Features

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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