research use only

lunresertib (RP-6306) PKMYT1 Inhibitor

Name: lunresertib (RP-6306)
SKU: E1175
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.E1175

Lunresertib (RP-6306) is a Protein Kinase, Membrane Associated Tyrosine/Threonine 1 (PKMYT1) inhibitor, and it can be used for the research of cancer.

Chemical Structure

Molecular Weight: 324.38

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.68%

99.68

Products Often Used Together with lunresertib (RP-6306)

Adavosertib (MK-1775)

It and Adavosertib use efficiently kills U2OS cells.

Dinaciclib

It is more cytotoxic to the CCNE1-amplified cell lines than dinaciclib.

Camonsertib (RP-3500)

It and RP-3500 are under clinical trial studies for their use in advanced solid tumors.

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 p21 BMI-1 LIM kinase Nur77 APC
Related Products	Adavosertib (MK-1775) PD0166285 Debio 0123 Azenosertib (Zn-C3) Phospho-Wee1 (Ser642) Antibody [P3A10] Wee1 Antibody [K14K15] Potrasertib

Chemical Information, Storage & Stability

Molecular Weight	324.38	Formula	C₁₈H₂₀N₄O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2719793-90-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (200.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL 65 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro	Lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. It shows a high degree of selectivity over other kinases in cellular binding assays.
In vivo	In a CCNE1-amplified ovarian xenograft model (OVCAR3), lunresertib (RP-6306) results in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth.
References	[1] https://pubmed.ncbi.nlm.nih.gov/35880755/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06107868	Active not recruiting	Recurrent Ovarian Cancer\|Recurrent Uterine Cancer\|Metastatic Cancer\|Advanced Cancer	University Health Network Toronto	March 20 2024	Phase 1
NCT05147350	Active not recruiting	Advanced Solid Tumor	Repare Therapeutics	August 9 2022	Phase 1
NCT05147272	Active not recruiting	Adult Solid Tumor	Repare Therapeutics	December 16 2021	Phase 1
NCT04855656	Recruiting	Advanced Solid Tumor	Repare Therapeutics\|Debiopharm International SA	April 30 2021	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):