(Rac)-lunresertib
Based on 1 Customer Validation
(Rac)-lunresertib (compound 181) is a potent membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor with an IC50 of <10 nM. (Rac)-lunresertib (compound 181) has anticancer effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.72%
- CAS. Nr.: 2719749-28-5
- Formel: C18H20N4O2
- Molecular Weight:324.38
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
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PKMYT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1569 | IC50 |
0.06 μM
Compound: 4; RP-6306
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Antiproliferative activity against human HCC1569 cells incubated for 48 to 96 hrs by CCK-8 assay
Antiproliferative activity against human HCC1569 cells incubated for 48 to 96 hrs by CCK-8 assay
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[PMID: 39163619] |
| HCC1569 | IC50 |
0.15 μM
Compound: RP-6306
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Antiproliferative activity against human HCC1569 cells assessed as inhibition of cell growth incubated for 7 days by CTG assay
Antiproliferative activity against human HCC1569 cells assessed as inhibition of cell growth incubated for 7 days by CTG assay
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[PMID: 38146659] |
| OVCAR-3 | EC50 |
0.2 nM
Compound: RP-6306
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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
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[PMID: 35880755] |
| ZR-75-1 | IC50 |
14.02 μM
Compound: 4; RP-6306
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Antiproliferative activity against human ZR-75-1 cells incubated for 48 to 96 hrs by CCK-8 assay
Antiproliferative activity against human ZR-75-1 cells incubated for 48 to 96 hrs by CCK-8 assay
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[PMID: 39163619] |
Chemical Information
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CAS. Nr. 2719749-28-5
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Appearance Solid
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Molecular Weight 324.38
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Formel C18H20N4O2
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Color Off-white to yellow
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SMILES
O=C(C1=C(N)N(C2=C(C)C(O)=CC=C2C)C3=NC(C)=C(C)C=C31)N
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Synonyms
(Rac)-RP-6306
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (308.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (3.08 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (3.08 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
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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