2. Stem Cell/Wnt Autophagy
  3. BMI1 Autophagy
  4. PTC-209

PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment.

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 : 315704-66-6

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 96 在庫あり
Solution
10 mM * 1 mL in DMSO USD 96 在庫あり
Solid
5 mg $88 在庫あり
10 mg $154 在庫あり
25 mg $315 在庫あり
50 mg $500 在庫あり
100 mg $650 在庫あり
200 mg   お問い合わせ  
500 mg   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 16 publication(s) in Google Scholar

Other Forms of PTC-209:

PTC-209 関連抗体

Top Publications Citing Use of Products

    PTC-209 purchased from MedChemExpress. Usage Cited in: Oncogene. 2020 Jan;39(1):17-29.  [Abstract]

    BMI1 inhibitor delays CRPC progression in vivo. C4-2 cells are treated with PTC209.

    PTC-209 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Feb 5;9(1):500.  [Abstract]

    BMI1-specific antagonist inhibits androgen receptor (AR)-signaling pathway. C4-2 or 22Rv1 is treated with PTC209 in indicated concentration for 48 h, BMI1 and AR are tested by western blot, and GAPDH served as loading control.

    PTC-209 purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2017 May 4;20(5):621-634.e6.  [Abstract]

    The Combination Therapy of Cisplatin Plus PTC-209 Potently Eradicates Bmi1+ CSCs and Inhibits Tumor Progression by Lineage Tracing. Western blots show that Bmi1 is reduced in tumors treated with PTC-209.

    • 生物活性

    • 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

    PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment[1][2].

    IC50 & Target

    IC50: 0.5 μM (BMI-1, in HT1080 tumor cells)[1]
    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    0.65 nM
    Compound: PTC-209
    Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
    		[PMID: 30429953]
    HCT-116 IC50
    0.7 μM
    Compound: PTC-209
    Inhibition of Bmi1 protein expression in human HCT116 cells after 8 hrs by Western blot analysis
    Inhibition of Bmi1 protein expression in human HCT116 cells after 8 hrs by Western blot analysis
    		[PMID: 30429953]
    HCT-8 IC50
    0.59 μM
    Compound: PTC-209
    Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay
    Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay
    		[PMID: 30429953]
    HT-29 IC50
    0.61 μM
    Compound: PTC-209
    Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay
    		[PMID: 30429953]
    体外実験

    PTC-209 (0.01-10 μM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested[2].
    PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells[2].

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

    PTC-209 関連抗体

    Cell Viability Assay[2]

    Cell Line: Lung (LNM35, A549 cells), breast (MDA-MB-231 and T47D cells), and colon (HT-29, HCT-116, and HCT8/S11 cells)
    Concentration: 0.01-10 µM
    Incubation Time: 24, 48, and 72 hour
    Result: Induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested.
    体内実験

    PTC-209 (60 mg/kg body weight; subcutaneously; once a day for 11 days) significantly reduces tumor volume[1].

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

    Animal Model: Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor)[1]
    Dosage: 60 mg/kg body weight
    Administration: Subcutaneously; once a day for 11 days
    Result: Significantly reduced tumor volume
    分子量

    495.19

    分子式

    C17H13Br2N5OS
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    CC1=C(C2=CSC(NC3=C(Br)C=C(OC)C=C3Br)=N2)N4C=CC=NC4=N1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 32 mg/mL (64.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0194 mL 10.0971 mL 20.1943 mL
    5 mM 0.4039 mL 2.0194 mL 4.0389 mL
    10 mM 0.2019 mL 1.0097 mL 2.0194 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. 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

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    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.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.76%

    COA (254 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    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. 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 2.0194 mL 10.0971 mL 20.1943 mL 50.4857 mL
    5 mM 0.4039 mL 2.0194 mL 4.0389 mL 10.0971 mL
    10 mM 0.2019 mL 1.0097 mL 2.0194 mL 5.0486 mL
    15 mM 0.1346 mL 0.6731 mL 1.3463 mL 3.3657 mL
    20 mM 0.1010 mL 0.5049 mL 1.0097 mL 2.5243 mL
    25 mM 0.0808 mL 0.4039 mL 0.8078 mL 2.0194 mL
    30 mM 0.0673 mL 0.3366 mL 0.6731 mL 1.6829 mL
    40 mM 0.0505 mL 0.2524 mL 0.5049 mL 1.2621 mL
    50 mM 0.0404 mL 0.2019 mL 0.4039 mL 1.0097 mL
    60 mM 0.0337 mL 0.1683 mL 0.3366 mL 0.8414 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.

    PTC-209 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:

    PTC-209315704-66-6PTC209PTC 209BMI1AutophagyBmi-1B cell-specific Moloney murine leukemia virus integration site 1cancer-initiatingcellsCICsanti-myelomaHEK293TlungcolonbreasttumorInhibitorinhibitorinhibit

    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:
    PTC-209
    製品番号:
    HY-15888
    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.