2. Epigenetics TGF-beta/Smad
  3. PKC
  4. Darovasertib

Darovasertib  (Synonyms: LXS196; IDE196)

Cat. No.: HY-101569 Purity: 99.78%
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SDS
Handling Instructions Technical Support

LXS196 est un inhibiteur de la protéine kinase C (PKC) qui est puissant, sélectif et oralement actif , avec des valeurs IC50 de 1,9 nM, 0,4 nM et 3,1 μM pour PKCα, PKCθ et GSK3β , respectivement. LXS196 a le potentiel pour la recherche sur le mélanome uvéal.

Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research.

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

CAS No. : 1874276-76-2

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Customer Review

Based on 4 publication(s) in Google Scholar

Darovasertib Related Antibodies

Top Publications Citing Use of Products

    Darovasertib purchased from MedChemExpress. Usage Cited in: Patent. US20210230154A1.

    Darovasertib (0-10 μM) inhibited 92-1 cells growth in a dose-dependent manner.

    Darovasertib purchased from MedChemExpress. Usage Cited in: Patent. US20210230154A1.

    Darovasertib (0-10 μM) inhibited MP-14 cells growth in a dose-dependent manner.

    View All PKC Isoform Specific Products:

    View All Isoforms
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research[1][2].

    IC50 & Target[2]

    PKCα

    1.9 nM (IC50)

    PKCθ

    0.4 nM (IC50)

    GSK3β

    3.1 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    SK-MEL-28 IC50
    > 10 μM
    Compound: 20; LXS196
    Cytotoxicity against human SK-MEL-28 cells expressing B-Raf V600E mutant
    Cytotoxicity against human SK-MEL-28 cells expressing B-Raf V600E mutant
    		[PMID: 38198520]
    In Vitro

    Upon oral administration, protein kinase C inhibitor Darovasertib (LXS196) binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival[1].

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

    Darovasertib Related Antibodies
    In Vivo

    Darovasertib (LXS196; compound 9) (15, 30, 75, 150 mg/kg, P.O., mice) shows improved efficacy (regression) in a 92.1 GNAQ uveal melanoma xenograft model in a dose-dependently manner[2].

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

    Animal Model: Mice implanted with 92.1 GNAQ mutant uveal melanoma cells[2].
    Dosage: 15, 30, 75, 150 mg/kg
    Administration: P.O. (bid) for 35 days
    Result: Dose-dependently suppressed the tumor growth.
    Clinical Trial
    Molecular Weight

    472.47

    Formula

    C22H23F3N8O
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    NC1=C(C(NC2=C(N3CCC(C)(N)CC3)C=CC=N2)=O)N=C(C4=NC=CC=C4C(F)(F)F)C=N1
    Shipping

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

    DMSO : 25 mg/mL (52.91 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 2.1165 mL 10.5827 mL 21.1654 mL
    5 mM 0.4233 mL 2.1165 mL 4.2331 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
    =
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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

    ×
    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 (5.29 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 (5.29 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: 99.78%

    SDS (393 KB)

    COA (255 KB) HNMR (277 KB) RP-HPLC (232 KB) LCMS (330 KB)

    Handling Instructions (2659 KB)
    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, 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 2.1165 mL 10.5827 mL 21.1654 mL 52.9134 mL
    5 mM 0.4233 mL 2.1165 mL 4.2331 mL 10.5827 mL
    10 mM 0.2117 mL 1.0583 mL 2.1165 mL 5.2913 mL
    15 mM 0.1411 mL 0.7055 mL 1.4110 mL 3.5276 mL
    20 mM 0.1058 mL 0.5291 mL 1.0583 mL 2.6457 mL
    25 mM 0.0847 mL 0.4233 mL 0.8466 mL 2.1165 mL
    30 mM 0.0706 mL 0.3528 mL 0.7055 mL 1.7638 mL
    40 mM 0.0529 mL 0.2646 mL 0.5291 mL 1.3228 mL
    50 mM 0.0423 mL 0.2117 mL 0.4233 mL 1.0583 mL
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    Darovasertib 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:

    Darovasertib1874276-76-2LXS196 IDE196LXS 196LXS-196IDE196IDE 196IDE-196PKCProtein kinase CInhibitorinhibitorinhibit

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