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Biological Activity

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

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

In Vivo
In vivo	RP-6306 results in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth in CCNE1-amplified ovarian xenograft model (OVCAR3).

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

[1] Szychowski J, et al. J Med Chem. 2022 Aug 11;65(15):10251-10284.

Chemical Information & Solubility

Molecular Weight	324.38	Formula	C₁₈H₂₀N₄O₂
CAS No.	2719793-90-3	SDF	--
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 65 mg/mL ( (200.38 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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+ %

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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