1. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  2. ATM/ATR
  3. Elimusertib

Elimusertib  (Synonyms: BAY 1895344)

製品番号: HY-101566 純度: 99.73%
COA 取扱説明書 Technical Support

Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity. Elimusertib can be used for the research of solid tumors and lymphomas.

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CAS 番号 : 1876467-74-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
5 mg $90 在庫あり
10 mg $140 在庫あり
25 mg $280 在庫あり
50 mg $460 在庫あり
100 mg $730 在庫あり
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カスタマーレビュー

Based on 15 publication(s) in Google Scholar

Other Forms of Elimusertib:

Top Publications Citing Use of Products

    Elimusertib purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2025 Feb;57(1):167-183.  [Abstract]

    Effects of Elimusertib on p-BRCA1 (s1423), BRCA1, and RAD51 protein levels. The cells were treated with 0.2 μM Elimusertib for 24 h, and Western blotting was used to detect protein expression. GAPDH was used as the internal control. All FHIT-deficient cells are marked in red.

    Elimusertib purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 May 6:102129.  [Abstract]

    Comparison of synergy scores for cisplatin by target drug. The Bliss score was calculated using SynergyFinder to evaluate the synergistic effects of BAY1895344 (0.01 μM; 5 days), AZD7762, EPZ015666, or everolimus in combination with cisplatin across 27 OSCC organoids, comprising 10 normal-like, 8 dense, and 9 grape-like subtypes.

    Elimusertib purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2024 Mar;25(3):1469-1489.  [Abstract]

    Cell viability assays in HCT116 and HT-29 cancer cells cultured at pH 7.4 or 6.5, and treated with the indicated doses of ATRi Elimusertib (0.03-1 μM) for 72 h.

    Elimusertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 24;15(1):9195.  [Abstract]

    PIDD1−/− HeLa cells transfected with indicated FLAG-PIDD1 variants with or without ATR inhibitor BAY 1895344 (BAY, 0.75 mM)were harvested at 24 h, immunoprecipitated with anti-PIDD1 pT788 antibody, and analyzed by western blot.

    Elimusertib purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 May:211:115494.  [Abstract]

    Elimusertib (10 μM; 1 h) pretreatment inhibits Ara-C-induced p38 MAPK phosphorylation but does not inhibit AKT dephosphorylation.

    ATM/ATR アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • 純度とドキュメンテーション

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    製品説明

    Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity[1][2]. Elimusertib can be used for the research of solid tumors and lymphomas[3].

    IC50 & Target[1]

    ATR

    7 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.09 3
    Compound: BAY1895344
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    [PMID: 35191694]
    A549 IC50
    0.09 3
    Compound: BAY1895344
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    [PMID: 35191694]
    A549 IC50
    0.09 3
    Compound: BAY1895344
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    [PMID: 35191694]
    SU-DHL-8 IC50
    9 1
    Compound: BAY-1895344
    Antiproliferative activity against human SUDHL8 cells assessed as reduction in cell viability measured after 4 days by celltiter-glo luminescent assay
    Antiproliferative activity against human SUDHL8 cells assessed as reduction in cell viability measured after 4 days by celltiter-glo luminescent assay
    [PMID: 32502336]
    HEK293 IC50
    > 10 3
    Compound: BAY-1895344
    Inhibition of recombinant human ERG stably expressed in HEK293 cells at -80 mV by whole cell voltage clamp method
    Inhibition of recombinant human ERG stably expressed in HEK293 cells at -80 mV by whole cell voltage clamp method
    [PMID: 32502336]
    HEK293 IC50
    > 10 3
    Compound: BAY-1895344
    Inhibition of recombinant human ERG stably expressed in HEK293 cells at -80 mV by whole cell voltage clamp method
    Inhibition of recombinant human ERG stably expressed in HEK293 cells at -80 mV by whole cell voltage clamp method
    [PMID: 32502336]
    HT-29 IC50
    160 1
    Compound: BAY-1895344
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    [PMID: 32502336]
    SU-DHL-8 IC50
    9 1
    Compound: 8
    Antiproliferative activity against human SU-DHL-8 cells measured after 72 to 96 hrs by CellTiter-Glo cell viability assay
    Antiproliferative activity against human SU-DHL-8 cells measured after 72 to 96 hrs by CellTiter-Glo cell viability assay
    [PMID: 33135887]
    HT-29 IC50
    160 1
    Compound: BAY-1895344
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    [PMID: 32502336]
    HT-29 IC50
    36 1
    Compound: BAY-1895344
    Inhibition of ATR in human HT-29 cells assessed as reduction in histone H2AX phosphorylation measured after 30 mins by immunofluorescence cytometric assay
    Inhibition of ATR in human HT-29 cells assessed as reduction in histone H2AX phosphorylation measured after 30 mins by immunofluorescence cytometric assay
    [PMID: 32502336]
    HEK293 IC50
    >10 3
    Compound: BAY-1895344
    Inhibition of recombinant human ERG stably expressed in HEK293 cells at -80 mV by whole cell voltage clamp method
    Inhibition of recombinant human ERG stably expressed in HEK293 cells at -80 mV by whole cell voltage clamp method
    [PMID: 32502336]
    HT-29 IC50
    36 1
    Compound: BAY-1895344
    Inhibition of ATR in human HT-29 cells assessed as reduction in histone H2AX phosphorylation measured after 30 mins by immunofluorescence cytometric assay
    Inhibition of ATR in human HT-29 cells assessed as reduction in histone H2AX phosphorylation measured after 30 mins by immunofluorescence cytometric assay
    [PMID: 32502336]
    LoVo IC50
    71 1
    Compound: BAY-1895344
    Antiproliferative activity against human LoVo cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    Antiproliferative activity against human LoVo cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    [PMID: 32502336]
    MCF7 IC50
    35 1
    Compound: BAY-1895344
    Inhibition of PI3K/AKT/mTOR signaling pathway in human MCF7 cells assessed as reduction in AKT phosphorylation at Ser473 residues measured after 30 mins by HTRF assay
    Inhibition of PI3K/AKT/mTOR signaling pathway in human MCF7 cells assessed as reduction in AKT phosphorylation at Ser473 residues measured after 30 mins by HTRF assay
    [PMID: 32502336]
    MCF7 IC50
    35 1
    Compound: BAY-1895344
    Inhibition of PI3K/AKT/mTOR signaling pathway in human MCF7 cells assessed as reduction in AKT phosphorylation at Ser473 residues measured after 30 mins by HTRF assay
    Inhibition of PI3K/AKT/mTOR signaling pathway in human MCF7 cells assessed as reduction in AKT phosphorylation at Ser473 residues measured after 30 mins by HTRF assay
    [PMID: 32502336]
    HT-29 IC50
    36 1
    Compound: BAY-1895344
    Inhibition of ATR in human HT-29 cells assessed as reduction in histone H2AX phosphorylation measured after 30 mins by immunofluorescence cytometric assay
    Inhibition of ATR in human HT-29 cells assessed as reduction in histone H2AX phosphorylation measured after 30 mins by immunofluorescence cytometric assay
    [PMID: 32502336]
    LoVo IC50
    0.041 3
    Compound: 5; BAY1895334
    Antiproliferative activity against human LoVo cells incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human LoVo cells incubated for 72 hrs by CCK-8 assay
    [PMID: 37130473]
    SU-DHL-8 IC50
    9 1
    Compound: 8
    Antiproliferative activity against human SU-DHL-8 cells measured after 72 to 96 hrs by CellTiter-Glo cell viability assay
    Antiproliferative activity against human SU-DHL-8 cells measured after 72 to 96 hrs by CellTiter-Glo cell viability assay
    [PMID: 33135887]
    LoVo IC50
    0.041 3
    Compound: 5; BAY1895334
    Antiproliferative activity against human LoVo cells incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human LoVo cells incubated for 72 hrs by CCK-8 assay
    [PMID: 37130473]
    SU-DHL-8 IC50
    9 1
    Compound: BAY-1895344
    Antiproliferative activity against human SUDHL8 cells assessed as reduction in cell viability measured after 4 days by celltiter-glo luminescent assay
    Antiproliferative activity against human SUDHL8 cells assessed as reduction in cell viability measured after 4 days by celltiter-glo luminescent assay
    [PMID: 32502336]
    LoVo IC50
    71 1
    Compound: BAY-1895344
    Antiproliferative activity against human LoVo cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    Antiproliferative activity against human LoVo cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    [PMID: 32502336]
    LoVo IC50
    27 1
    Compound: 4
    Cytotoxicity against human LoVo cells assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo assay
    Cytotoxicity against human LoVo cells assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo assay
    [PMID: 38299539]
    HT-29 IC50
    160 1
    Compound: BAY-1895344
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    [PMID: 32502336]
    LoVo IC50
    71 1
    Compound: BAY-1895344
    Antiproliferative activity against human LoVo cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    Antiproliferative activity against human LoVo cells assessed as reduction in cell viability measured after 4 days by crystal violet staining based assay
    [PMID: 32502336]
    MCF7 IC50
    35 1
    Compound: BAY-1895344
    Inhibition of PI3K/AKT/mTOR signaling pathway in human MCF7 cells assessed as reduction in AKT phosphorylation at Ser473 residues measured after 30 mins by HTRF assay
    Inhibition of PI3K/AKT/mTOR signaling pathway in human MCF7 cells assessed as reduction in AKT phosphorylation at Ser473 residues measured after 30 mins by HTRF assay
    [PMID: 32502336]
    SU-DHL-8 IC50
    9 1
    Compound: 8
    Antiproliferative activity against human SU-DHL-8 cells measured after 72 to 96 hrs by CellTiter-Glo cell viability assay
    Antiproliferative activity against human SU-DHL-8 cells measured after 72 to 96 hrs by CellTiter-Glo cell viability assay
    [PMID: 33135887]
    SU-DHL-8 IC50
    9 1
    Compound: BAY-1895344
    Antiproliferative activity against human SUDHL8 cells assessed as reduction in cell viability measured after 4 days by celltiter-glo luminescent assay
    Antiproliferative activity against human SUDHL8 cells assessed as reduction in cell viability measured after 4 days by celltiter-glo luminescent assay
    [PMID: 32502336]
    体外実験

    Elimusertib potently inhibits the proliferation of a broad spectrum of human tumor cell lines with a median IC50 of 78 nM[1].
    Elimusertib potently suppresses hydroxyurea-induced H2AX phosphorylation (IC50: 36 nM)[1].
    Elimusertib shows good selectivity against mTOR (ratio of IC50 values: mTOR/ATR 61)[3].
    Elimusertib reveals high selectivity against other related kinases, such as DNA-PK (IC50: 332 nM), ATM (IC50: 1420 nM), and PI3K (IC50: 3270 nM)[3].
    Elimusertib has potent antiproliferative activity against various cancer cell lines in vitro, 25 for example in the CRC cell lines HT-29 (IC50: 160 nM) and LoVo (IC50: 71 nM), and in the B-cell lymphoma cell line SU-DHL-8 (IC50: 9 nM)[3].

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

    体内実験

    Elimusertib shows potent anti-tumor efficacy in monotherapy in a variety of xenograft models of ovarian and colorectal cancer, and causes complete tumor remission in mantle cell lymphoma models[2].
    Elimusertib (50 mg/kg; p.o.; b.i.d.; 3 days on/4 days off; for 11 days) exhibits strong antitumor efficacy in the ATM-mutated SU-DHL-8 (ATM K1964E) human GCB-DLBCL cell line derived xenograft model in mice[3].
    Elimusertib (20 mg/kg, and 10 mg/kg from day 14; p.o.; daily; 2 days on/5 days off; for 42 days) in combination with Carboplatin (40 mg/kg; i.p.; daily; 1 day on/6 days off) results in synergistic antitumor activity in the platinum-resistant ATM protein low expressing CR5038 human CRC PDX model in NOD/SCID mice[3].
    Elimusertib exhibits moderate oral bioavailability (rat 87%, dog 51%) following oral administration (rat and dog 0.6-1 mg/kg)[3].
    Elimusertib exhibits terminal elimination half-lives (mouse 0.17 h, rat 1.3 and, dog 1.0 h) due to plasma clearance (3.5, 1.2, and 0.79 L/h/kg respectively) following intravenous administration (mouse, rat and dog 0.3-0.5 mg/kg)[3].

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

    Animal Model: Female C.B-17 SCID mice, SU-DHL-8 GCB-DLBCL xenograft model[3]
    Dosage: 50 mg/kg
    Administration: Oral administration, b.i.d., 3 days on/4 days off, for 11 days
    Result: Inhibited tumor area.
    Animal Model: Male Wistar rats[3]
    Dosage: 0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis)
    Administration: Intravenous injection and oral administration
    Result: Oral bioavailability (87%), T1/2 (1.3 h).
    Animal Model: Female beagle dogs[3]
    Dosage: 0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis)
    Administration: Intravenous injection and oral administration
    Result: Oral bioavailability (51%), T1/2 (1.0 h).
    分子量

    375.43

    分子式

    C20H21N7O

    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CN1N=CC=C1C2=C(C=CN=C3C4=CC=NN4)C3=NC(N5[C@H](C)COCC5)=C2

    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 : 5.4 mg/mL (14.38 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 2.6636 mL 13.3181 mL 26.6361 mL
    5 mM 0.5327 mL 2.6636 mL 5.3272 mL
    10 mM 0.2664 mL 1.3318 mL 2.6636 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

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    一般には略語で表示されます:C1V1 = C2V2

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    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    90% (20% SBE-β-CD in Saline)

      Solubility: 1.09 mg/mL (2.90 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.09 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 (10.9 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.
    • Protocol 2

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

      Solubility: 0.89 mg/mL (2.37 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 0.89 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 (8.9 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  0.5% CMC-Na/saline water

      Solubility: 4 mg/mL (10.65 mM); Suspended solution; Need ultrasonic and adjust pH to 3 with HCl

    In Vivo Dissolution Calculator
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    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).
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    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: 99.91%

    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 2.6636 mL 13.3181 mL 26.6361 mL 66.5903 mL
    5 mM 0.5327 mL 2.6636 mL 5.3272 mL 13.3181 mL
    10 mM 0.2664 mL 1.3318 mL 2.6636 mL 6.6590 mL
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    一般には略語で表示されます:C1V1 = C2V2

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    製品名:
    Elimusertib
    製品番号:
    HY-101566
    数量:
    MCE 日本正規代理店: