Art. -Nr.: HY-145817A

lunresertib

(Synonyms: RP-6306)

9 Cited Publications

Kundenbewertung

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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Reinheit: 99.97%
CAS. Nr.: 2719793-90-3
Formel: C₁₈H₂₀N₄O₂
Molecular Weight:324.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

lunresertib Chemical Structure

CAS. Nr.: 2719793-90-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PKMYT1

14 nM (IC₅₀)

Alle Wee1 Isoform-spezifische Produkte anzeigen :

PKMYT1

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2719793-90-3
Appearance Solid
Molecular Weight 324.38
Formel C₁₈H₂₀N₄O₂
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
Synonyms

RP-6306
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (9)

All Cell Proliferation/Viability AssayWBFlow Cytometry

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Journal Impact Factor

Signal Transduct Target Ther

PKMYT1 kinase ameliorates cisplatin sensitivity in osteosarcoma. [Abstract]

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.
Nature

Targeting G1-S-checkpoint-compromised cancers with cyclin A/B RxL inhibitors. [Abstract]

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.
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.
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

Cyclin A/B RxL Macrocyclic Inhibitors to Treat Cancers with High E2F Activity. [Abstract]

2024 Aug 1:2024.08.01.605889. PMID: 39211113

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0828 mL

15.4140 mL

30.8280 mL

5 mM

0.6166 mL

3.0828 mL

6.1656 mL

10 mM

0.3083 mL

1.5414 mL

3.0828 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

lunresertib

9 Cited Publications

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lunresertib

MCE Bioactive Compound Library

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Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) lunresertib

Alle Wee1 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

lunresertib

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) lunresertib

Alle Wee1 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

lunresertib Related Classifications

HY-145817A Related Classifications