2. Cell Cycle/DNA Damage
  3. Wee1
  4. lunresertib

lunresertib  (Synonyms: RP-6306)

Cat. No.: HY-145817A Purity: 99.90%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

lunresertib Chemical Structure

lunresertib Chemical Structure

CAS No. : 2719793-90-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 770 In-stock
Solution
10 mM * 1 mL in DMSO USD 770 In-stock
Solid
1 mg USD 280 In-stock
5 mg USD 700 In-stock
10 mg USD 1120 In-stock
25 mg USD 1580 In-stock
50 mg USD 2050 In-stock
100 mg USD 2650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Other Forms of lunresertib:

lunresertib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE lunresertib

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

IC50: 14 nM (PKMYT1)[1]
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.

lunresertib Related Antibodies
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
Molecular Weight

324.38

Formula

C18H20N4O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0828 mL 15.4140 mL 30.8280 mL
5 mM 0.6166 mL 3.0828 mL 6.1656 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    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.
  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.90%

COA (262 KB) HNMR (268 KB) RP-HPLC (255 KB) LCMS (130 KB)

Handling Instructions (2659 KB)
References

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
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lunresertib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

lunresertib2719793-90-3RP-6306RP6306RP 6306Wee1PKMYT1anticancer effectspan-γH2AXCDK1CCNE1Inhibitorinhibitorinhibit

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