2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. Dinaciclib

Dinaciclib  (Synonyms: SCH 727965)

Cat. No.: HY-10492 Purity: 99.36%
COA Handling Instructions

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Dinaciclib (SCH 727965) est un inhibiteur puissant de CDK, avec des IC50s de 1 nM, 1 nM, 3 nM et 4 nM pour CDK2, CDK5, CDK1 et CDK9, respectivement.

Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively.

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

Dinaciclib Chemical Structure

Dinaciclib Chemical Structure

CAS No. : 779353-01-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 144 In-stock
50 mg USD 468 In-stock
100 mg USD 660 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 43 publication(s) in Google Scholar

Dinaciclib Related Antibodies

Top Publications Citing Use of Products

41 Publications Citing Use of MCE Dinaciclib

Proliferation Assay
WB

    Dinaciclib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2020 Feb;19(2):627-636.  [Abstract]

    A2058 melanoma cells are treated with 50 nM Dinaciclib for 3 or 6 hours. Whole cell lysates are subjected to Western blotting (left).

    Dinaciclib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2020 Feb;19(2):627-636.  [Abstract]

    Human melanoma cells were treated with Dinaciclib at the indicated doses for 72 hours. After 72-hours incubation, cell viability is assessed by the CellTiter-Glo 2.0 assay. Relative growth to vehicle control is shown.

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively[1].

    IC50 & Target[1]

    CDK2

    1 nM (IC50)

    CDK5

    1 nM (IC50)

    CDK1

    3 nM (IC50)

    CDK9

    4 nM (IC50)

    In Vitro

    Dinaciclib (SCH 727965) is a potent DNA replication inhibitor that blocks thymidine (dThd) DNA incorporation in A2780 cells with an IC50 of 4 nM. Dinaciclib (100 nM) inhibits phosphorylation of the retinoblastoma (Rb) tumor suppressor protein and induces accumulation of the p85 PARP caspase cleavage product[1]. In vitro cell growth of pancreatic cancer cells is inhibited by Dinaciclib (SCH727965) in a dose-dependent manner. Upon incubation with Dinaciclib for 72 h, the GI50s are approximately 10 and 20 nM for MIAPaCa-2 and Pa20C cells, respectively. These results are consistent with studies of Dinaciclib in other cancer cell lines. In soft agar assays, 5 to 10 nM of Dinaciclib significantly reduces colony formation and anchorage independent growth of MIAPaCa-2 cells. Moreover, in vitro cell migration of Pa20C and MIAPaCa-2 cells is significantly reduced by Dinaciclib-concentrations starting from 2-5 nM, as demonstrated using BD FluoroChrom, modified Boyden Chamber and wound healing assays[2].

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

    Dinaciclib Related Antibodies
    In Vivo

    Dinaciclib (8, 16, 32, and 48 mg/kg, i.p.) results in tumor inhibition by 70%, 70%, 89%, and 96%, respectively; Dinaciclib (SCH 727965) is well tolerated, and the maximum body weight loss in the highest dosage group is 5%. Dinaciclib has a short plasma half-life in mouse. A dose of 5 mg/kg Dinaciclib given i.p. in mice is associated with a plasma half-life of ~0.25 hour[1]. Treatment with Dinaciclib (SCH727965) given as twice weekly i.p. doses of 40 mg/kg for 4 weeks causes significant tumor growth inhibition (TGI) in 10/10 (100%) of low-passage subcutaneous pancreatic xenografts tested[2].

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

    396.49

    Formula

    C21H28N6O2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    OCC[C@H]1N(CCCC1)C2=NC3=C(C=NN3C(NCC4=C[N+]([O-])=CC=C4)=C2)CC
    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 : 50 mg/mL (126.11 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 2.5221 mL 12.6107 mL 25.2213 mL
    5 mM 0.5044 mL 2.5221 mL 5.0443 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)

    Mass
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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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    Volume (final)

    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 (6.31 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 (6.31 mM); Suspended solution

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

    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:  20% HP-β-CD in Saline

      Solubility: 10 mg/mL (25.22 mM); Clear solution; Need ultrasonic

    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: 99.36%

    COA (254 KB) HNMR (166 KB) LCMS (120 KB)

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

    Recombinant cyclin/CDK holoenzymes are purified from Sf9 cells engineered to produce baculoviruses that express a specific cyclin or CDK. Cyclin/CDK complexes are typically diluted to a final concentration of 50 μg/mL in a kinase reaction buffer containing 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 1 mM DTT, and 0.1 mM sodium orthovanadate. For each kinase reaction, 1 μg of enzyme and 20 μL of a 2 μM substrate solution (a biotinylated peptide derived from histone H1) are mixed and combined with 10 μL of diluted Dinaciclib (SCH 727965). The reaction is started by the addition of 50 μL of 2 μM ATP and 0.1 μCi of 33P-ATP. Kinase reactions are incubated for 1 hour at room temperature and are stopped by the addition of 0.1% Triton X-100, 1 mM ATP, 5 mM EDTA, and 5 mg/mL streptavidin-coated SPA beads. SPA beads are captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads are washed twice with 2 M NaCl and twice with 2 M NaCl containing 1% phosphoric acid. The signal is then assayed using a TopCount 96-well liquid scintillation counter. Dose-response curves are generated from duplicate, eight-point serial dilutions of inhibitory compounds. IC50 values are derived by nonlinear regression analysis[1].

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

    A2780 cells are plated onto tissue culture dishes and propagated with the appropriate growth media. Growing cultures are exposed to increasing concentrations of Dinaciclib (0.75, 1.5, 3.15, 6.25, 12.5, 25, and 500 nM) or a vehicle control, typically for 7 days. After removing the medium, cells are fixed with 50% methanol/50% acetone for 5 minutes and stained with 0.2% crystal violet in 2% ethanol for 5 minutes. Following staining, cells are washed with 5 to 10 mL of water. Stained cells are solubilized in 1% deoxycholic acid, and the absorbance of the resulting solution is measured at 600 nm using a SOFTmax PRO 4.3 plate reader. Absorbance of Dinaciclib-treated samples is plotted as a percent of that of a vehicle-treated control, and data are reported as an IC50 value relative to these controls. For suspension cell lines, assessments of cell viability are obtained using the alamarBlue Cell Viability Assay kit[1].

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

    Mice[1]
    For tumor implantation, specific cell lines are grown in vitro, washed once with PBS, and resuspended in 50% Matrigel in PBS to a final concentration of 4×107 to 5×107 cells per milliliter. Nude mice are injected with 0.1 mL of this suspension s.c. in the flank region. Tumor length (L), width (W), and height (H) are measured by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L×W×H)/2. When the tumor volume reaches 100 mm3, the animals are randomized to treatment groups (10 mice/group) and treated i.p. with either Dinaciclib (8, 16, 32, and 48 mg/kg daily, i.p.) or individual chemotherapeutic agents according to the dosing schedule indicated in table and figure legends. Tumor volumes and body weights are measured during and after the treatment periods.

    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 2.5221 mL 12.6107 mL 25.2213 mL 63.0533 mL
    5 mM 0.5044 mL 2.5221 mL 5.0443 mL 12.6107 mL
    10 mM 0.2522 mL 1.2611 mL 2.5221 mL 6.3053 mL
    15 mM 0.1681 mL 0.8407 mL 1.6814 mL 4.2036 mL
    20 mM 0.1261 mL 0.6305 mL 1.2611 mL 3.1527 mL
    25 mM 0.1009 mL 0.5044 mL 1.0089 mL 2.5221 mL
    30 mM 0.0841 mL 0.4204 mL 0.8407 mL 2.1018 mL
    40 mM 0.0631 mL 0.3153 mL 0.6305 mL 1.5763 mL
    50 mM 0.0504 mL 0.2522 mL 0.5044 mL 1.2611 mL
    60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0509 mL
    80 mM 0.0315 mL 0.1576 mL 0.3153 mL 0.7882 mL
    100 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6305 mL
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    Dinaciclib 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:

    Dinaciclib779353-01-4SCH 727965SCH727965SCH-727965CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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