1. Epigenetics PROTAC
  2. Epigenetic Reader Domain Ligands for Target Protein for PROTAC
  3. BI-7273

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.

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The BI-7273 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

CAS 番号 : 1883429-21-7

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 97 在庫あり
Solution
10 mM * 1 mL in DMSO USD 97 在庫あり
Solid
5 mg $89 在庫あり
10 mg $140 在庫あり
25 mg $290 在庫あり
50 mg $465 在庫あり
100 mg $744 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of BI-7273:

Top Publications Citing Use of Products

    BI-7273 purchased from MedChemExpress. Usage Cited in: Noncoding RNA. 2025 Apr 29;11(3):33.

    Treatment with Bi7273 (5 μM) is ineffective in modulating cell adhesion molecules E-cadherin and β4 integrin, while it can downregulate a known BRD7/BRD9 target gene like CCND1.
    • 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

    BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.

    IC50 & Target

    BRD9

     

    Cellular Effect
    Cell Line Type Value Description References
    A204 IC50
    0.3717 μM
    Compound: 1a;BI-7273
    Antiproliferative activity against human A204 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay
    Antiproliferative activity against human A204 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay
    [PMID: 30540463]
    EOL1 EC50
    1400 nM
    Compound: 1; BI-7273
    Antiproliferative activity against human EOL-1 cells by cell titre glo assay
    Antiproliferative activity against human EOL-1 cells by cell titre glo assay
    [PMID: 26914985]
    EOL1 IC50
    0.08926 μM
    Compound: 1a;BI-7273
    Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay
    Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay
    [PMID: 30540463]
    G-401 IC50
    4.9 μM
    Compound: 3; BI-7273
    Inhibition of cell viability in human G-401 cells incubated for 4 days by CellTiter-Glo luminescent cell viability assay
    Inhibition of cell viability in human G-401 cells incubated for 4 days by CellTiter-Glo luminescent cell viability assay
    [PMID: 39132814]
    体外実験

    BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM. BI-7273 also has slight activity against a panel of kinases such as CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2) and TAF1L(2), with Kds of 8.8 nM, 210 nM, 2600 nM, 8600 nM, 10000 nM, 850 nM, 1000 nM, and 1200 nM, respectively. BI-7273 (1 μM) is active in U2OS cell lines. BI-7273 blocks EOL-1 cell proliferation with EC50 of 1400 nM[1].

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

    分子量

    353.41

    分子式

    C20H23N3O3

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CN(C)CC1=C(OC)C=C(C(C2=C3C=NC=C2)=CN(C)C3=O)C=C1OC

    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 : 10 mg/mL (28.30 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 2.8296 mL 14.1479 mL 28.2957 mL
    5 mM 0.5659 mL 2.8296 mL 5.6591 mL
    10 mM 0.2830 mL 1.4148 mL 2.8296 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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: ≥ 1 mg/mL (2.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1 mg/mL (2.83 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 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 (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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: 99.75%

    参考文献
    キナーゼ実験
    [1]

    His-tagged BRD9 is immobilized to a density of 2000-4000 RUs on flow cells 3 and 4 of a Biacore NTA-chip. Carbonic anhydrase II is immobilized at a similar density on flow cell 2 and a blank reference surface is generated on flow cell 1. The buffer is then switched to assay buffer (HBS-P+ = 10 mM HEPES, pH 7.4, 150 mM NaCl, 0.05 % P20 + 5 % DMSO) and the chip equilibrated for several hours before use for Kd determinations. To be able to correct for differences in bulk solvent refractive index caused by small variations in the DMSO concentration solvent correction samples are included at the beginning and end of the run. Compounds (BI-7273, etc.) are injected in concentration series (1:1 dilutions, 7 different concentrations), starting with a maximum concentration that is approximately 10-20-fold higher than the expected Kd. The concentration series are prepared in 96-well plates. In the case that the dilution window chosen for a particular compound does not appropriately bracket the Kd of the compound the measurement is repeated with an optimized starting concentration. Positive and negative control samples are included at regular intervals to be able to monitor the performance of the assay. CBS is used as a positive control for carbonic anhydrase II to check for integrity of the reference protein at regular intervals. To correct for the excluded volume effect a DMSO calibration series is prepared and the calibration samples are measured at the beginning and end of each run. Kd values are determined and averaged[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。

    細胞実験
    [1]

    Cells are grown in 50 µL medium for 7 days starting with 500 and with 1000 cells per well of a 384 well plate in the presence of varying concentrations of compound (BI-7273, etc.) before measuring viability via cellular ATP levels using the cell titer glow assay[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。

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8296 mL 14.1479 mL 28.2957 mL 70.7394 mL
    5 mM 0.5659 mL 2.8296 mL 5.6591 mL 14.1479 mL
    10 mM 0.2830 mL 1.4148 mL 2.8296 mL 7.0739 mL
    15 mM 0.1886 mL 0.9432 mL 1.8864 mL 4.7160 mL
    20 mM 0.1415 mL 0.7074 mL 1.4148 mL 3.5370 mL
    25 mM 0.1132 mL 0.5659 mL 1.1318 mL 2.8296 mL
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    • 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.

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    Inquiry Information

    製品名:
    BI-7273
    製品番号:
    HY-100351
    数量:
    MCE 日本正規代理店: