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lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects.

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CAS No. : 2719793-90-3

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 7 publication(s) in Google Scholar

Other Forms of lunresertib:

lunresertib Related Antibodies

Top Publications Citing Use of Products

    lunresertib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 May 21;10(1):165.  [Abstract]

    HOS and 143B cells were treated with or without Iunresertib (RP-6306) (2 μM; 24 h), and cells were harvested for co-immunoprecipitation experiments followed by western blot analysis. Iunresertib (RP-6306) inhibited activity of PKMYT1 and significantly reduced NPM1 phosphorylation.

    lunresertib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 May 21;10(1):165.  [Abstract]

    Iunresertib (RP-6306) (2 μM; 24 h) notably decreased NPM1 S260 phosphorylation levels in HOS, 143B and U2OS cells.

    lunresertib purchased from MedChemExpress. Usage Cited in: Nature. 2025 Oct;646(8085):734-745.  [Abstract]

    The MYT1 inhibitor Iunresertib (RP-6306) (100 nM; 5 d) potentiated cell killing by CIRc-018 in NCI-H1048 cells.

    lunresertib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jul 15;16(1):526.  [Abstract]

    Iunresertib (RP-6306) (0.01-100 μM;48 h) markedly inhibited the growth of Panc-1, MiaPaCa-2, BxPC-3, and AsPC-1 cells, , with IC50 values ranging from 0.554 to 1.435 μM.

    lunresertib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jul 15;16(1):526.  [Abstract]

    Iunresertib (RP-6306) (0.4-1.4 μM; 48 h) instigated a cell cycle arrest, predominantly augmenting the proportion of cells in the G2/M phase and eliciting a conspicuous surge in S phase cells in MiaPaCa-2.

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    PKMYT1

    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects[1].

    IC50 & Target

    PKMYT1

    14 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    OVCAR-3 EC50
    0.2 nM
    Compound: RP-6306
    In vivo inhibition of PKMYT1 in SCID/Beige mouse xenografted with human OVCAR-3 cells assessed as inhibition of CDK1 phosphorylation measured upto 10 hrs post oral dose by ELISA method
    In vivo inhibition of PKMYT1 in SCID/Beige mouse xenografted with human OVCAR-3 cells assessed as inhibition of CDK1 phosphorylation measured upto 10 hrs post oral dose by ELISA method
    		[PMID: 35880755]
    In Vitro

    lunresertib (500 nM; for 24 h) treatment induces pan-γH2AX in an HCC1569 breast cancer cell line, indicating that tumour-derived CCNE1 amplification also renders cells vulnerable to DNA damage induction following PKMYT1 inhibition[2].
    lunresertib treatment causes unscheduled activation of CDK1 selectively in CCNE1-overexpressing cells, promoting early mitosis in cells undergoing DNA synthesis[2].

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

    lunresertib Related Antibodies
    In Vivo

    lunresertib (15, 50, and 300 ppm; oral; daily; for 21 days) results in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth in CCNE1-amplified ovarian xenograft model (OVCAR3)[1].

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

    Animal Model: OVCAR3-bearing mice[1]
    Dosage: 15, 50, and 300 ppm (equivalent to approximately 3, 10, and 60 mg/kg/day)
    Administration: Oral; daily; for 21 days
    Result: Resulted in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth.
    Clinical Trial
    분자량

    324.38

    화학식

    C18H20N4O2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to gray

    SMILES

    O=C(C1=C(N)[N@]([C@]2=C(C)C(O)=CC=C2C)C3=NC(C)=C(C)C=C31)N
    선적

    Room temperature in continental US; may vary elsewhere.
    보관
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    용액&용해도
    In Vitro: 

    DMSO : 50 mg/mL (154.14 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 3.0828 mL 15.4140 mL 30.8280 mL
    5 mM 0.6166 mL 3.0828 mL 6.1656 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.

    • 몰농도 계산기

    • 농도 희석 계산기

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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    90% (20% SBE-β-CD in Saline)

      Solubility: 5 mg/mL (15.41 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (7.71 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.
    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.
    순도&문서

    Purity: 99.97%

    SDS (252 KB)

    COA (262 KB) HNMR (303 KB) RP-HPLC (266 KB) LCMS (93 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, 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 3.0828 mL 15.4140 mL 30.8280 mL 77.0701 mL
    5 mM 0.6166 mL 3.0828 mL 6.1656 mL 15.4140 mL
    10 mM 0.3083 mL 1.5414 mL 3.0828 mL 7.7070 mL
    15 mM 0.2055 mL 1.0276 mL 2.0552 mL 5.1380 mL
    20 mM 0.1541 mL 0.7707 mL 1.5414 mL 3.8535 mL
    25 mM 0.1233 mL 0.6166 mL 1.2331 mL 3.0828 mL
    30 mM 0.1028 mL 0.5138 mL 1.0276 mL 2.5690 mL
    40 mM 0.0771 mL 0.3854 mL 0.7707 mL 1.9268 mL
    50 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5414 mL
    60 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.2845 mL
    80 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9634 mL
    100 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
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    lunresertib 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:

    lunresertib2719793-90-3RP-6306RP6306RP 6306Wee1PKMYT1anticancer effectspan-γH2AXCDK1CCNE1Inhibitorinhibitorinhibit

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    Cat. No.:
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