lunresertib
Based on 9 publication(s) in Google Scholar
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.97%
- CAS 番号: 2719793-90-3
- 分子式: C18H20N4O2
- 分子量:324.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 lunresertib
More- Signal Transduct Target Ther. 2025 May 21;10(1):165. [Abstract]
- Nature. 2025 Oct;646(8085):734-745. [Abstract]
- Cell Death Dis. 2025 Jul 15;16(1):526. [Abstract]
- Oncogene. 2026 Jun 10. [Abstract]
- Oncogene. 2025 Dec;44(50):4868-4877. [Abstract]
- J Inflamm Res. 2025 Jul 26:18:10029-10049. [Abstract]
- bioRxiv. 2026 Apr 13:2026.04.11.717899. [Abstract]
- bioRxiv. 2025 Nov 4:2025.11.03.686258. [Abstract]
- bioRxiv. 2024 Aug 1:2024.08.01.605889. [Abstract]
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Flow Cytometry
生物活性
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PKMYT1 14 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| OVCAR-3 | EC50 |
0.2 nM
Compound: RP-6306
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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
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[PMID: 35880755] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OVCAR3-bearing mice[1]
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Dosage:15, 50, and 300 ppm (equivalent to approximately 3, 10, and 60 mg/kg/day)
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Administration:Oral; daily; for 21 days
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Result:Resulted in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2719793-90-3
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性状 Solid
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分子量 324.38
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分子式 C18H20N4O2
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Color Off-white to gray
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SMILES
O=C(C1=C(N)[N@]([C@]2=C(C)C(O)=CC=C2C)C3=NC(C)=C(C)C=C31)N
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別名
RP-6306
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
2025 May 21;10(1):165. PMID: 40393983
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.
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Nature
2025 Oct;646(8085):734-745. PMID: 40836083
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.
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Cell Death Dis
Targeted delivery of the PKMYT1 inhibitor RP-6306 mediates PANoptosis in pancreatic cancer via mitotic catastrophe. [Abstract]2025 Jul 15;16(1):526. PMID: 40664640
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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Oncogene
DNA replication stress and translational repression converge to drive CDK1- and caspase-dependent apoptosis in Ewing sarcoma. [Abstract]2026 Jun 10. PMID: 42270776 -
Oncogene
Targeting FZD6 creates therapeutically actionable vulnerabilities for advanced prostate cancer. [Abstract]2025 Dec;44(50):4868-4877. PMID: 41286306 -
J Inflamm Res
Multi-Omics Analysis Combined with Machine Learning Identified FABP4 in Smooth Muscle Cells as a Pathogenic Factor in Atherosclerosis. [Abstract]2025 Jul 26:18:10029-10049. PMID: 40740974 -
bioRxiv
ARID1A deficiency unleashes centromeric RNA transcription to drive chromosomal instability and boosts PKMYT1 inhibitor efficacy via RNA sensing. [Abstract]2026 Apr 13:2026.04.11.717899. PMID: 42039593 -
bioRxiv
Mitotic bypass and endocycling promote cancer cell survival after genotoxic chemotherapy. [Abstract]2025 Nov 4:2025.11.03.686258. PMID: 41278999 -
bioRxiv
2024 Aug 1:2024.08.01.605889. PMID: 39211113
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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データシート (285 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Janek Szychowski, et al. Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 2022 Aug 11;65(15):10251-10284. [Content Brief]
[2]. David Gallo, et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature. 2022 Apr;604(7907):749-756. [Content Brief]
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 |
lunresertib 関連分類
HY-145817A 関連分類
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