2. Cell Cycle/DNA Damage Autophagy
  3. Checkpoint Kinase (Chk) Autophagy
  4. Rabusertib

Rabusertib  (Synonyms: LY2603618; IC-83)

Cat. No.: HY-14720 Purity: 99.99%
COA Handling Instructions

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Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.

For research use only. We do not sell to patients.

Rabusertib Chemical Structure

Rabusertib Chemical Structure

CAS No. : 911222-45-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 53 In-stock
Solution
10 mM * 1 mL in DMSO USD 53 In-stock
Solid
5 mg USD 48 In-stock
10 mg USD 73 In-stock
25 mg USD 146 In-stock
50 mg USD 220 In-stock
100 mg USD 330 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Rabusertib Related Antibodies

Top Publications Citing Use of Products

    Rabusertib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023, 15(3), 850.

    Prexasertib (5 µM; 24 h) decreases CHK1 expression in HepG2 and Huh-7 cells and increases γ-H2AX level.

    View All Checkpoint Kinase (Chk) Isoform Specific Products:

    View All Isoforms
    Chk1 Chk2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.

    IC50 & Target

    Chk1

    7 nM (IC50)

    Chk2

    12000 nM (IC50)

    PDK1

    893 nM (IC50)

    CAMK2

    1550 nM (IC50)

    VEGFR3

    2128 nM (IC50)

    MET

    2200 nM (IC50)

    JNK1

    4930 nM (IC50)

    RSK2

    5700 nM (IC50)

    NTRK1

    12000 nM (IC50)

    In Vitro

    Rabusertib (LY2603618) is a highly effective inhibitor of multiple aspects of Chk1 biology. Rabusertib (LY2603618) is tested against a panel of 51 diverse protein kinases in vitro. With an IC50 of 7 nM for Chk1, Rabusertib (LY2603618) is approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated (PDK1, IC50=893 nM, others >1000 nM). Rabusertib (LY2603618) effectively reduced Chk1 autophosphorylation with an EC50 of 430 nM. Inhibition of Chk1 by Rabusertib (LY2603618) also effectively abrogated the G2/M DNA damage checkpoint in cells treated with DNA damaging agents. Treatment of cells with Rabusertib (LY2603618) produced a cellular phenotype similar to that reported for depletion of Chk1 by RNAi. Inhibition of intracellular Chk1 by Rabusertib (LY2603618) results in impaired DNA synthesis, elevated H2A.X phosphorylation indicative of DNA damage and premature entry into mitosis[1]. Treatments of the SK-N-BE(2) cells with variable concentrations of Rabusertib (LY2603618) results in dose-dependent inhibition of cell growth determined by MTT assays with an IC50 of 10.81 µM[1].

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

    Rabusertib Related Antibodies
    In Vivo

    Mice bearing Calu-6 xenografts are treated with 150 mg/kg (IP) Gemcitabine and a single simultaneous 200 mg/kg oral dose of Rabusertib (LY2603618). 200 mg/kg of Rabusertib (LY2603618) is sufficient to inhibit 85 % of Chk1 autophosphorylation in vivo at 2 h. Rabusertib (LY2603618) effectively reduces Gemcitabine-induced phosphorylation on Tlk serine 695 as well, supporting the cited report with a selective chemical inhibitor of Chk1[1].

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

    436.30

    Formula

    C18H22BrN5O3
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    BrC(C=C1NC(NC2=NC=C(N=C2)C)=O)=C(C=C1OC[C@H]3OCCNC3)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 31.25 mg/mL (71.63 mM; ultrasonic and warming and heat to 60°C; 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 2.2920 mL 11.4600 mL 22.9200 mL
    5 mM 0.4584 mL 2.2920 mL 4.5840 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    V2

    In Vivo:

    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 (5.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    Purity & Documentation

    Purity: 99.99%

    COA (250 KB) HNMR (527 KB) RP-HPLC (258 KB) LCMS (130 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cells are plated at 2.5×103 per well, on 96-well tissue culture plates and incubated for one cell doubling (18-24 h). Gemcitabine dilutions are set up by half-log steps across a final concentration range of 1-1000 nM. Rabusertib (LY2603618) is prepared by dilutions in DMSO to 5000× final concentration, and then diluted 1000-fold into medium to generate 5× stocks for addition to wells. Approximately 24 h after Gemcitabine addition, Rabusertib (LY2603618) is added. Each combination is done in triplicate. After a period of two cell doublings following Rabusertib (LY2603618) addition, MTS/PMS reagent is added to each well according to the manufacturer’s instructions. Absorbance is read on a Spectra Max 250 spectrophotometer at 490 nm and the data analyzed with GraphPad Prism 4.0. Dose-response curves are fit by non-linear regression, with bottom fits constrained to 0 % inhibition[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Female Harlan athymic nude mice (26-28 g) are used for these studies. Tumor growth is initiated by subcutaneous injection of 1×106 Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm3 in size, the animals are randomized by tumor size and body weight, and placed into their respective treatment groups. Each animal receives 2 injections, one of either saline vehicle or 150 mg/kg Gemcitabine administered by intraperitoneal injection in a volume of 200 μL, and the other being the Captisol vehicle or LY2603618 administered orally in a volume of 200 μL.

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

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2920 mL 11.4600 mL 22.9200 mL 57.3000 mL
    5 mM 0.4584 mL 2.2920 mL 4.5840 mL 11.4600 mL
    10 mM 0.2292 mL 1.1460 mL 2.2920 mL 5.7300 mL
    15 mM 0.1528 mL 0.7640 mL 1.5280 mL 3.8200 mL
    20 mM 0.1146 mL 0.5730 mL 1.1460 mL 2.8650 mL
    25 mM 0.0917 mL 0.4584 mL 0.9168 mL 2.2920 mL
    30 mM 0.0764 mL 0.3820 mL 0.7640 mL 1.9100 mL
    40 mM 0.0573 mL 0.2865 mL 0.5730 mL 1.4325 mL
    50 mM 0.0458 mL 0.2292 mL 0.4584 mL 1.1460 mL
    60 mM 0.0382 mL 0.1910 mL 0.3820 mL 0.9550 mL
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    Rabusertib Related Classifications

    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:

    Rabusertib911222-45-2LY2603618 IC-83LY 2603618LY-2603618IC83IC 83IC-83Checkpoint Kinase (Chk)AutophagyInhibitorinhibitorinhibit

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