(S)-Navlimetostat
Based on 1 Customer Validation
(S)-Navlimetostat (example 16-7) is the S-enantiomer of Navlimetostat. (S)-Navlimetostat is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM.
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- Purity: 98.15%
- CAS No.: 2630904-44-6
- 화학식: C23H18ClFN6O2
- 분자량:464.88
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
>10 μM
Compound: (P)-27
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Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
|
[PMID: 35041419] |
| HCT-116 | IC50 |
890 nM
Compound: (M)-27; MRTX1719
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Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
|
[PMID: 35041419] |
| HCT-116 | IC50 |
12 nM
Compound: MRTX1719
|
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as cell viability after 10 days by CellTiter-Glo assay
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as cell viability after 10 days by CellTiter-Glo assay
|
[PMID: 35926325] |
| HCT-116 | IC50 |
890 nM
Compound: MRTX1719
|
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as cell viability after 10 days by CellTiter-Glo assay
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as cell viability after 10 days by CellTiter-Glo assay
|
[PMID: 35926325] |
| HepG2 | IC50 |
6600 nM
Compound: MRTX1719
|
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability measured after 120 hrs CellTiter-Glo assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability measured after 120 hrs CellTiter-Glo assay
|
[PMID: 35926325] |
Chemical Information
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CAS No. 2630904-44-6
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Appearance Solid
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분자량 464.88
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화학식 C23H18ClFN6O2
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Color White to off-white
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SMILES
FC1=C(C=C(C(C#N)=[C@@]1[C@@]2=C(C3=CC=C4C(C(CN)=NNC4=O)=C3)C=NN2C)OC5CC5)Cl
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Synonyms
(S)-MRTX-1719; (S)-BMS-986504
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (215.11 mM; Need ultrasonic; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 5 mg/mL (10.76 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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 | 2.1511 mL | 10.7555 mL | 21.5109 mL | 53.7773 mL |
| 5 mM | 0.4302 mL | 2.1511 mL | 4.3022 mL | 10.7555 mL | |
| 10 mM | 0.2151 mL | 1.0755 mL | 2.1511 mL | 5.3777 mL | |
| 15 mM | 0.1434 mL | 0.7170 mL | 1.4341 mL | 3.5852 mL | |
| 20 mM | 0.1076 mL | 0.5378 mL | 1.0755 mL | 2.6889 mL | |
| 25 mM | 0.0860 mL | 0.4302 mL | 0.8604 mL | 2.1511 mL | |
| 30 mM | 0.0717 mL | 0.3585 mL | 0.7170 mL | 1.7926 mL | |
| 40 mM | 0.0538 mL | 0.2689 mL | 0.5378 mL | 1.3444 mL | |
| 50 mM | 0.0430 mL | 0.2151 mL | 0.4302 mL | 1.0755 mL | |
| 60 mM | 0.0359 mL | 0.1793 mL | 0.3585 mL | 0.8963 mL | |
| 80 mM | 0.0269 mL | 0.1344 mL | 0.2689 mL | 0.6722 mL | |
| 100 mM | 0.0215 mL | 0.1076 mL | 0.2151 mL | 0.5378 mL |