2. Antibody-drug Conjugate/ADC Related Cell Cycle/DNA Damage
  3. ADC Payload Topoisomerase
  4. Exatecan

Exatecan  (Synonyms: DX-8951)

製品番号: HY-13631 純度: 99.78% ee.: 99.16%
COA 取扱説明書 Technical Support

Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 171335-80-1

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 49 在庫あり
Solution
10 mM * 1 mL in DMSO USD 49 在庫あり
Solid
5 mg $45 在庫あり
10 mg $60 在庫あり
25 mg $120 在庫あり
50 mg $172 在庫あり
100 mg $255 在庫あり
250 mg $390 在庫あり
500 mg $540 在庫あり
1 g $780 在庫あり
5 g $1950 在庫あり
10 g   お問い合わせ  
50 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 23 publication(s) in Google Scholar

Other Forms of Exatecan:

Exatecan 関連抗体

Top Publications Citing Use of Products

    Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2025 Oct 13;24(1):253.  [Abstract]

    Western blot analysis of B1-5V (BRCA1-) and B2-4V (BRCA2-) cells treated with PBS (NT, no treatment), V66-exatecan (100 nM) ADC for 1-24 h, or V66 alone (24 h). In samples treated with V66-exatecan ADC, a time-dependent accumulation of DNA damage is observed, as indicated by the increased γH2AX and pATM signals, along with a time-dependent down-regulation of TOP1.

    Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027.  [Abstract]

    In vivo efficacy of AMT-562, Ab562-T1000-Exatecan (10 mg/kg; i.v.), and P-GGFG-DXd in PC9 xenograft model.

    Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027.  [Abstract]

    In vitro cytotoxicity of Exatecan and DXd in HER3-expressing cells. Cells were incubated with a concentration series of Exatecan or DXd for 5 days. Cell viability was measured by CCK-8 and IC50 for each cell line was calculated from cell viability-concentration plot.

    Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027.  [Abstract]

    Representative hematoxylin and eosin staining of toxicity organs of AMT-562 and Ab562-T1000-Exatecan (ADC; 30 mg/kg; i.v.). Scale bar, 200 mm.

    Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027.  [Abstract]

    Single dose pharmacokinetic profiles of AMT-562 (ADC) and Ab562-GGFG-DXd in mice. ADCs were intravenously administered to mice at the dose of 10 mg/kg.

    Exatecan purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027.  [Abstract]

    Patient-derived colon cancer organoids response to AMT-562 (ADC) and P-GGFG-DXd. Representative images of brightfield (left) and live/dead cells (right) for CO117 was shown. Colon cancer PDOs were treated with AMT-562 or P-GGFG-DXd at a serial concentration for 6 days. Live cells were stained by Calcein AM (green) and dead cells by PI (red).

    Exatecan purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2021 Mar 9;14(3):247.  [Abstract]

    Tra-Exa-PSAR10 and Tra-Exa-PSAR0 (0.01-10 nM, 6 days). In vitro cytotoxicity of ADCs in breast and gastric HER2+ and HER2- (MCF-7) cancer cell lines after 6-day exposure to trastuzumab conjugates, as assayed by MTT assay, n = 3.

    ADC Payload アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Auristatin Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

    Topoisomerase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Topoisomerase Topo I Topo II DNA gyrase

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.

    IC50 & Target[1]

    Camptothecins

     

    体外実験

    Exatecan is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI50s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively[1]. Exatecan Mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respctively. Exatecan Mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Exatecan 関連抗体
    体内実験

    Exatecan Mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death[1]. Exatecan Mesylate (15, 25 mg/kg, i.v.) hightly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan Mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    435.45

    分子式

    C24H22FN3O4
    CAS 番号
    Appearance

    Solid

    Color

    Yellow to brown

    SMILES

    O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5N)C(C)=C(F)C=C6N=C4C3=C2)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    -20°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    DMSO : 20 mg/mL (45.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2965 mL 11.4824 mL 22.9647 mL
    5 mM 0.4593 mL 2.2965 mL 4.5929 mL
    10 mM 0.2296 mL 1.1482 mL 2.2965 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    純度とドキュメンテーション

    純度: 99.93%

    COA (257 KB) HNMR (282 KB) RP-HPLC (255 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験

    sup>[3]Cells (5×106) are lysed with SDS buffer (10 mM HEPES, 2 mM orthovanadate, 10 mM NaF, 10 mM pyrophosphate, 1 mMPMSF, 10 µg/mL leupeptin, 10% 2-mercaptoethanol, 10% glycerol,8% SDS, 42 mM Tris-HCl, 0.002% bromophenol blue, pH 7.4). Protein in the whole cell lysates is separated in 7.5% polyacryl-amide gel and blotted onto nitrocellulose membrane. The membrane is treated with anti-Topo I human antibody and subsequently, with horseradish peroxidase-conjugated protein A. The Topo I-specific band is detected with ECL reagents. To obtain a nuclear extract, cells (5×107) are washed with ice-cold buffer (2 mM K2HPO4, 5 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 0.1 mM dithiothreitol), resuspended in buffer containing 0.35% Triton-X100 and PMSF and then incubated on ice for 10 min. The resulting lysates are centrifuged, and precipitates are then incubated with buffer containing 0.35 M NaCl for 1 hr at 4°C. After centrifugation (18,000g, 10 min), the protein concentration of the supernatant (nuclear extract) is determined by Bradford’s method using a protein assay kit. The same amount of nuclear protein is analyzed by Western blotting analysis using anti-Topo I antibody[3].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [1]

    Growth inhibition experiments are carride out in 96-well flat-bottomed microplates, and the amount of viable cell at the end of the incubation is determined by MTT assay. Thus, 500-20000 cells/well in 150 μL of medium are plated and grown for 24 h (P388, CCRF-CEM and K562 cells for 4h), the drug (including Exatecan Mesylate, in 150 μL medium/well), or the medium alone as a control, is added, and the cells are cultured for an additional 3 days. After addition of MTT (20 μL/well, 5 mg/mL in phosphate-buffered saline), the plates are incubated for 4 h and centrifuged at 800 g for 5 min, then the medium is removed and the blue dye formed is dissolved in 150 μL of DMSO. the absorbance is measured at 540 nm using a Microplate Reader model 3550[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [2]

    At 3 weeks after BxPC-3-GFP and MIA-PaCa-2-GFP orthotopic implantation, mice are randomized into five different groups of 5 mice each for treatment purposes. Group 1 serves as the negative control and does not receive any treatment. Groups 2 and 3 are treated with Exatecan Mesylate at 25 and 15 mg/kg/dose, respectively. Groups 4 and 5 receive gemcitabine treatments at 300 and 150 mg/kg/dose, respectively. At 6 weeks after BxPC-3-GFP orthotopic implantation, mice are randomized into three different groups of 20 mice each for treatment purposes. Group 1 serves as the negative control and does not receive any treatment. Group 2 is treated with 25 mg/kg/dose Exatecan Mesylate and group 3 receives 300 mg/kg/dose gemcitabine. Dosing for both drugs is performed once a week for 3 weeks, discontinued for 2 weeks, and then continued for another 3 weeks. In both early and late cancer models, primary tumor size and body weights are measured once a week. Tumor volumes are calculated using the formula a × b2 × 0.5, where a and b represent the larger and smaller diameters, respectively. At the termination of the studies, mice are sacrificed and explored. Final tumor weights and direct GFP images of primary tumor and metastases are recorded for each mouse. The tumor growth IR is calculated using the formula IR (%) = (1 − TWt/TWc) × 100, where TWt and TWc are the mean tumor weight of treated and control groups, respectively[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2965 mL 11.4824 mL 22.9647 mL 57.4119 mL
    5 mM 0.4593 mL 2.2965 mL 4.5929 mL 11.4824 mL
    10 mM 0.2296 mL 1.1482 mL 2.2965 mL 5.7412 mL
    15 mM 0.1531 mL 0.7655 mL 1.5310 mL 3.8275 mL
    20 mM 0.1148 mL 0.5741 mL 1.1482 mL 2.8706 mL
    25 mM 0.0919 mL 0.4593 mL 0.9186 mL 2.2965 mL
    30 mM 0.0765 mL 0.3827 mL 0.7655 mL 1.9137 mL
    40 mM 0.0574 mL 0.2871 mL 0.5741 mL 1.4353 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Exatecan Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Exatecan171335-80-1DX-8951DX8951DX 8951ADC PayloadTopoisomeraseADC CytotoxinInhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

    		  

    カスタマ需要量 *

    お名前 *

    		 

    タイトル

    メールアドレス *

    		 

    電話番号 *

    デパートメント

    		 

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

    		      

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Exatecan
    製品番号:
    HY-13631
    数量:
    MCE 日本正規代理店:

    カスタマーレビュー

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    製品名

    		  

    Lot #

    お名前 *

    		 

    メールアドレス *

    電話番号 *

    		 

    部門 *

    組纖名 *

    		 

    国或いは地域 *

    備考

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.