Rinzimetostat
Based on 1 publication(s) in Google Scholar
Rinzimetostat (ORIC-944) is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.
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- Pureza: 99.90%
- No. CAS: 2369769-29-7
- Fòrmula: C26H25FN6O
- Peso molecular:456.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) Rinzimetostat
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
polycomb repressive complex 2; PRC2[1]
Rinzimetostat (ORIC-944) (30 mg/kg; op; everyday for 30 days) demonstrates strong single agent activity to enzalutamide in prostate cancer xenograft model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KARPAS-422 DLBCL xenograft model[1]
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Dosage:30, 100, 200 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Had well tolerated at all dose levels assessed compared to tazemetostat at a clinically relevant dose.
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Animal Model:22Rv1 model
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Dosage:30 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Made average tumor volume ± SEM, with n=8-10/group.
Had a significant difference in ORIC-944 treatment group vs vehicle.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2369769-29-7
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Appearance Solid
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Peso molecular 456.51
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Fòrmula C26H25FN6O
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Color White to off-white
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SMILES
CC1=C(C=CC(CN(C)C)=C1)C2=CN=C(N3C=C(N=C23)C#N)NCC4=C(C=CC5=C4CCO5)F
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Synonyms
ORIC-944
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 100 mg/mL (219.05 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 (5.48 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.
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.1905 mL | 10.9527 mL | 21.9053 mL | 54.7633 mL |
| 5 mM | 0.4381 mL | 2.1905 mL | 4.3811 mL | 10.9527 mL | |
| 10 mM | 0.2191 mL | 1.0953 mL | 2.1905 mL | 5.4763 mL | |
| 15 mM | 0.1460 mL | 0.7302 mL | 1.4604 mL | 3.6509 mL | |
| 20 mM | 0.1095 mL | 0.5476 mL | 1.0953 mL | 2.7382 mL | |
| 25 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1905 mL | |
| 30 mM | 0.0730 mL | 0.3651 mL | 0.7302 mL | 1.8254 mL | |
| 40 mM | 0.0548 mL | 0.2738 mL | 0.5476 mL | 1.3691 mL | |
| 50 mM | 0.0438 mL | 0.2191 mL | 0.4381 mL | 1.0953 mL | |
| 60 mM | 0.0365 mL | 0.1825 mL | 0.3651 mL | 0.9127 mL | |
| 80 mM | 0.0274 mL | 0.1369 mL | 0.2738 mL | 0.6845 mL | |
| 100 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.5476 mL |
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