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RP-6306

Name: RP-6306
Brand: TargetMol
SKU: T60889
Price: 133 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T60889Cas No. 2719793-90-3

Lunresertib (RP-6306) is a potent, selective, and orally active PKMYT1 inhibitor with an IC50 of 14 nM. Lunresertib (RP-6306) inhibits the growth of CCNE1-amplified tumor cells in several preclinical xenograft models.

RP-6306

🥰Excellent

Purity: 99.28%

Catalog No. T60889Cas No. 2719793-90-3

Pack Size	Price	Availability
1 mg	$133	In Stock
5 mg	$329	In Stock
10 mg	$488	In Stock
25 mg	$786	In Stock
50 mg	$1,090	In Stock
1 mL x 10 mM (in DMSO)	$587	In Stock

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Purity:99.28%

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	Lunresertib (RP-6306) is a potent, selective, and orally active PKMYT1 inhibitor with an IC50 of 14 nM. Lunresertib (RP-6306) inhibits the growth of CCNE1-amplified tumor cells in several preclinical xenograft models.
Targets&IC50	CDK1-pT14 cells:7.5 ± 1.8 nM, CDK1-pY15 cells:> 2 μM, PKMYT1:14 nM
In vitro	METHODS: HCC1569 breast cancer cell line was treated with lunresertib (RP-6306) (63, 125, 250, 500 nM) to assess whether PKMYT1 inhibition leads to DNA damage in CCNE1-high cells by monitoring γH2AX levels using quantitative image-based flow cytometry. RESULTS Treatment with lunresertib (RP-6306) induced pan-γH2AX in the HCC1569 breast cancer cell line, suggesting that tumor-derived CCNE1 amplification also renders cells susceptible to DNA damage induction following PKMYT1 inhibition. [1]
In vivo	METHODS: lunresertib (RP-6306) (3, 10 and 60 mg/kg, oral, daily) was used to treat CCNE1-amplified ovary xenograft model (OVCAR3) mice, and tumor growth in the mice was observed. RESULTS lunresertib (RP-6306) inhibited tumor growth in OVCAR3 mice in a statistically significant concentration-dependent manner. [2]

Chemical Properties

Molecular Weight	324.38
Formula	C₁₈H₂₀N₄O₂
Cas No.	2719793-90-3
Smiles	NC=1N(C=2C(C1C(N)=O)=CC(C)=C(C)N2)C3=C(C)C(O)=CC=C3C
Color	Yellow
Appearance	Solid

Storage & Solubility Information

Storage

keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 67.3 mg/mL (207.47 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.17 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0828 mL	15.4140 mL	30.8280 mL	154.1402 mL
5 mM	0.6166 mL	3.0828 mL	6.1656 mL	30.8280 mL
10 mM	0.3083 mL	1.5414 mL	3.0828 mL	15.4140 mL
20 mM	0.1541 mL	0.7707 mL	1.5414 mL	7.7070 mL
50 mM	0.0617 mL	0.3083 mL	0.6166 mL	3.0828 mL
100 mM	0.0308 mL	0.1541 mL	0.3083 mL	1.5414 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc