Vopimetostat
Based on 1 Customer Validation
TNG-462 is an orally active and selective PRMT5 inhibitor with anti-tumor activity against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation cancers.
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- Purity: 99.55%
- CAS No.: 2760483-96-1
- 화학식: C28H36N6O2S
- 분자량:520.69
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
More
Biological Activity
PRMT5[1].
TNG-462 (0-1 μM) exhibits selectivity and inhibition of cell viability in MTAP deficient tumor cells (NSCLC, PDAC, bladder, hematological malignancies), with IC50values less than 1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MTAP gene knockout (HCT116) or by reconstituting exogenous MTAP in an endogenous MTAP-deleted cell line (LN18)
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Concentration:0-1 μM
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Incubation Time:7 days
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Result:Selectively and specifically inhibited the cell viability of MTAP deficient cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LU99 MTAP-null cell line-derived xenograft mice model[1].
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Dosage:40, 100 mg/kg
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Administration:Oral gavage (p.o.); once daily (100 mg/kg) or b.i.d (40 mg/kg); 21 days
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Result:Inhibited the growth of tumor volume.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2760483-96-1
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Appearance Solid
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분자량 520.69
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화학식 C28H36N6O2S
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Color White to off-white
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SMILES
CCC1=CC(NC(C(N2[C@@H](C3=CC=C(SC(C4CCN(CC4)C)=N5)C5=C3)CC[C@@H](C2)C)=O)=O)=CN=C1N
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Synonyms
TNG-462
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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 (192.05 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: ≥ 2.5 mg/mL (4.80 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.80 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 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.
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 (277 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)
- 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 | 1.9205 mL | 9.6026 mL | 19.2053 mL | 48.0132 mL |
| 5 mM | 0.3841 mL | 1.9205 mL | 3.8411 mL | 9.6026 mL | |
| 10 mM | 0.1921 mL | 0.9603 mL | 1.9205 mL | 4.8013 mL | |
| 15 mM | 0.1280 mL | 0.6402 mL | 1.2804 mL | 3.2009 mL | |
| 20 mM | 0.0960 mL | 0.4801 mL | 0.9603 mL | 2.4007 mL | |
| 25 mM | 0.0768 mL | 0.3841 mL | 0.7682 mL | 1.9205 mL | |
| 30 mM | 0.0640 mL | 0.3201 mL | 0.6402 mL | 1.6004 mL | |
| 40 mM | 0.0480 mL | 0.2401 mL | 0.4801 mL | 1.2003 mL | |
| 50 mM | 0.0384 mL | 0.1921 mL | 0.3841 mL | 0.9603 mL | |
| 60 mM | 0.0320 mL | 0.1600 mL | 0.3201 mL | 0.8002 mL | |
| 80 mM | 0.0240 mL | 0.1200 mL | 0.2401 mL | 0.6002 mL | |
| 100 mM | 0.0192 mL | 0.0960 mL | 0.1921 mL | 0.4801 mL |
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