CUDC-101

製品コードS1194

CUDC-101化学構造

分子量(MW):434.49

CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.

サイズ 価格(税別)  
JPY 26560.00
JPY 19920.00
JPY 78020.00

カスタマーフィードバック(3)

  • (a) Decay-corrected microPET/CT scan of MDA-MB-231 tumor bearing mice (n = 4) at 2, 4, and 24 h after i.v. injection of [64Cu]7. The image obtained with coinjection of CUDC-101 (20 mg/kg body weight) is shown for a 24 h blockade. Tumors are indicated by arrows. (b) Decay-corrected region-of interest (ROI) analysis on microPET images of the tumor uptake of [64Cu]7 with or without coinjection of CUDC-101 (20 mg/kg body weight). *, P < 0.05; **, P < 0.01.

    ACS Med Chem Lett 2013 4(9), 858-62. CUDC-101 purchased from Selleck.

    After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CUDC-101 for 3h,followed by 15-minute stimolation of 100ng/ml EGF

     

    Dr. Zhang of Tianjin Medical University. CUDC-101 purchased from Selleck.

  • Effect of CUDC-101 on the viability was detected by WST-1 method after 3 days treatment in endometrial cancer cell line Hec50 and lshikawa and ovarian cancer cell line SKOV3,Caov and PA-1.

     

     

    Dr. Xiangbing Meng of University of Iowa. CUDC-101 purchased from Selleck.

製品安全説明書

HDAC阻害剤の選択性比較

生物活性

製品説明 CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
ターゲット
EGFR [1]
(Cell-free assay)
HDAC [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC6 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
2.4 nM 4.4 nM 4.5 nM 5.1 nM 9.1 nM
体外試験

Specific for class I and class II HDACs, CUDC-101 does not inhibit class III Sir-type HDACs. CUDC-101 displays weak activity against other protein kinases including KDR/VEGFR2, Lyn, Lck, Abl-1, FGFR-2, Flt-3, and Ret with IC50 of 0.85 μM, 0.84 μM, 5.91 μM, 2.89 μM, 3.43 μM, 1.5 μM, abd 3.2 μM, respectively. CUDC-101 displays broad antiproliferative activity in many human cancer cell types with IC50 of 0.04-0.80 μM, exhibiting a higher potency than erlotinib, lapatinib, and combinations of vorinostat with either erlotinib or lapatinib in most cases. CUDC-101 potently inhibits lapatinib- and erlotinib-resistant cancer cell lines. [1] CUDC-101 inhibits the erlotinib-resistant EGFR mutant T790M although its effects are incomplete with an Amax of ~60% of peak enzyme activity after inhibition. CUDC-101 treatment increases the acetylation of histone H3 and H4, as well as the acetylation of non-histone substrates of HDAC such as p53 and α-tubulin, in a dose-dependant manner in various cancer cell lines. CUDC-101 also suppresses HER3 expression, Met amplification, and AKT reactivation in tumor cells. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SK-BR-3 cells NFnjXItRem:uaX\ldoF1cW:wIHHzd4F6 NFLZd3RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMWJTNTNiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTBwMESg{txO NHe4e2ozODF2M{e3PC=>
MDA-MB-231 cells Mk\PVJJwdGmoZYLheIlwdiCjc4PhfS=> NETqNWxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhcHK|IHL5JGFVWCClb370[Y51KGG|c3H5MEBKSzVyPUCuNUDPxE1? MVyyNFE1Ozd5OB?=
human HepG2 cells M1;qbXBzd2yrZnXyZZRqd25iYYPzZZk> MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKGi{czDifUBCXFBiY3;ueIVvfCCjc4PhfUwhUUN3ME2wMlE{KM7:TR?= NYG2bGFYOjBzNEO3O|g>
human SKHEP1 cells M1f4UHBzd2yrZnXyZZRqd25iYYPzZZk> MorsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1jFVFEh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvOjJizszN M2\CcFIxOTR|N{e4
human Hep3B2 cells NV7DSnN4WHKxbHnm[ZJifGmxbjDhd5NigQ>? Mk\kRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYCzRlIh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvOjNizszN Mm\3NlAyPDN5N{i=
human BxPC3 cells NGS3ZWNRem:uaX\ldoF1cW:wIHHzd4F6 M4PQ[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQojQR|Mh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvOjdizszN M1;5b|IxOTR|N{e4
human NCI-H358 cells NUPje4M5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NXfvPG1bSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDN3ODDj[YxteyCjZoTldkBpenNiYomgRXRRKGOxboTlcpQh[XO|YYmsJGlEPTB;MD60JO69VQ>? MkPjNlAyPDN5N{i=
human MCF7 cells NUfkTFlGWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhcHK|IHL5JGFVWCClb370[Y51KGG|c3H5MEBKSzVyPUCuOVUh|ryP M3W5V|IxOTR|N{e4
human HCC827 cells NYLpe3VWWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFQ{iyO{Bk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9NE43KM7:TR?= NXzQSZc6OjBzNEO3O|g>
human H460 cells NVH3VlB5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUi4c3hVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF0xNjdizszN NIWzbFczODF2M{e3PC=>
human Capan1 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 MoTaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFYYDhclEh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvQCEQvF2= M2S1VVIxOTR|N{e4

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 Administration of CUDC-101 at 120 mg/kg/day induces tumor regression in the Hep-G2 liver cancer model, which is more efficacious than that of erlotinib at its maximum tolerated dose (25 mg/kg/day) and vorinostat at an equimolar concentration dose (72 mg/kg/day). CUDC-101 inhibits the growth of erlotinib-sensitive H358 NSCLC xenografts in a dose-dependent manner. CUDC-101 also shows potent inhibition of tumor growth in the erlotinib-resistant A549 NSCLC xenograft model. CUDC-101 produces significant tumor regression in the lapatinib-resistant, HER2-negative, EGFR-overexpressing MDA-MB-468 breast cancer model and the EGFR-overexpressing CAL-27 head and neck squamous cell carcinoma (HNSCC) model. Additionally, CUDC-101 inhibits tumor growth in the K-ras mutant HCT116 colorectal and EGFR/HER2 (neu)-expressing HPAC pancreatic cancer models. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

HDAC, EGFR and HER2 inhibition assays:

The activities of Class I and II HDACs are assessed using the Biomol Color de Lys system. Briefly, HeLa cell nuclear extracts are used as a source of HDACs. Different concentrations of CUDC-101 are added to HeLa cell nuclear extracts in the presence of a colorimetric artificial substrate. Developer is added at the end of the assay and enzyme activity is measured in the Wallac Victor II 1420 microplate reader at 405 nM. EGFR and HER2 kinase activity are measured using HTScan EGF receptor and HER2 kinase assay kits. Briefly, the GST-EGFR fusion protein is incubated with synthetic biotinylated peptide substrate and varying concentrations of CUDC-101 in the presence of 400 mM ATP. Phosphorylated substrate is captured with strapavidin-coated 96-well plates. The level of phosphorylation is monitored by antiphospho-tyrosine- and europium-labeled secondary antibodies. The enhancement solution is added at the end of the assay and enzyme activity is measured in the Wallac Victor II 1420 microplate reader at 615 nM.
細胞試験: [1]
+ 展開
  • 細胞株: HCC827, H358, H460, HepG2, Hep3B2, Sk-Hep-1, Capan1, BxPc3, MCF-7, MDA-MB-231, and Sk-Br-3
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間: 72 hours
  • 実験の流れ: Cancer cell lines are plated at 5000 to 10000 cells per well in 96-well flatbottomed plates with varying concentrations of CUDC-101. The cells are incubated with CUDC-101 for 72 hours in the presence of 0.5% of fetal bovine serum. Growth inhibition is assessed by an adenosine triphosphate (ATP) content assay using the Perkin-Elmer ATPlite kit. Apoptosis is routinely assessed by measuring the activities of Caspase-3 and -7 using Apo-ONE Homogeneous Assay Kit.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: Female athymic mice (nude nu/nu CD-1) inoculated with Hep-G2, H358, A549, MDA-MB468, HCT116, CAL-27, HepG2, or HPAC
  • 製剤: Formulated in 30% Captisol solution
  • 投薬量: ~120 mg/kg/day
  • 投与方法: Administered via i.v.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 20 mg/mL (46.03 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
15% Captisol
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 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 434.49
化学式

C24H26N4O4

CAS No. 1012054-59-9
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 (g) = 濃度 (mol/L) x 体積 (L) 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

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01702285 Terminated Cancer Curis Inc. September 2012 Phase 1
NCT01702285 Terminated Cancer Curis Inc. September 2012 Phase 1
NCT01384799 Completed Head and Neck Cancer Curis Inc. November 2011 Phase 1
NCT01384799 Completed Head and Neck Cancer Curis Inc. November 2011 Phase 1
NCT01171924 Completed Head and Neck Cancer|Liver Cancer|Breast Cancer|Gastric Cancer|Non-Small Cell Lung Cancer Curis Inc. July 2010 Phase 1
NCT01171924 Completed Head and Neck Cancer|Liver Cancer|Breast Cancer|Gastric Cancer|Non-Small Cell Lung Cancer Curis Inc. July 2010 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

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

HDACシグナル伝達経路

HDAC 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