BMS-986470
Based on 1 Customer Validation
BMS-986470, a HbF-activating CRBN E3 ligase modulator (CELMoD), is an orally active dual molecular glue degrader targeting ZBTB7A and WIZ. BMS-986470 has potent γ-globin induction activity. BMS-986470 can be used for sickle cell disease (SCD) research.
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- Pureté : 99.78%
- CAS No.: 3036554-12-5
- Formule: C29H25N5O5
- Masse moléculaire:523.54
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vivo
BMS-986470 (daily for 16 days) induces dose-dependently degradation of WIZ and ZBTB7A, along with an increase in circulating immature erythrocytes, and increased HBG1/2 transcript, γ-globin protein and erythroid progenitor markers in the peripheral blood and bone marrow in healthy cynomolgus monkeys[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3036554-12-5
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Appearance Solid
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Masse moléculaire 523.54
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Formule C29H25N5O5
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Color Light yellow to yellow
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SMILES
CC1=NC=CC(C2=CC3=C(N(C(CC3)=O)C)C=C2NC4=CC=CC5=C4C(N(C5=O)[C@H]6CCC(NC6=O)=O)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (191.01 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (4.78 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:
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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.
Pureté et documentation
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Fiche technique (275 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 1.9101 mL | 9.5504 mL | 19.1007 mL | 47.7518 mL |
| 5 mM | 0.3820 mL | 1.9101 mL | 3.8201 mL | 9.5504 mL | |
| 10 mM | 0.1910 mL | 0.9550 mL | 1.9101 mL | 4.7752 mL | |
| 15 mM | 0.1273 mL | 0.6367 mL | 1.2734 mL | 3.1835 mL | |
| 20 mM | 0.0955 mL | 0.4775 mL | 0.9550 mL | 2.3876 mL | |
| 25 mM | 0.0764 mL | 0.3820 mL | 0.7640 mL | 1.9101 mL | |
| 30 mM | 0.0637 mL | 0.3183 mL | 0.6367 mL | 1.5917 mL | |
| 40 mM | 0.0478 mL | 0.2388 mL | 0.4775 mL | 1.1938 mL | |
| 50 mM | 0.0382 mL | 0.1910 mL | 0.3820 mL | 0.9550 mL | |
| 60 mM | 0.0318 mL | 0.1592 mL | 0.3183 mL | 0.7959 mL | |
| 80 mM | 0.0239 mL | 0.1194 mL | 0.2388 mL | 0.5969 mL | |
| 100 mM | 0.0191 mL | 0.0955 mL | 0.1910 mL | 0.4775 mL |
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