Cemsidomide
Based on 1 Customer Validation
Cemsidomide (CFT7455) is a ubiquitin ligase pathway based IKZF1/3 (Ikaros/Aiolos) degrader with molecular glue activity. Cemsidomide has a GI50 of 0.05 nM for NCIH929.1 cells. Cemsidomide is used in the research of multiple myeloma (MM).
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- Purity: 99.54%
- CAS No.: 2504235-67-8
- 화학식: C28H27N3O4
- 분자량:469.53
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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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Biological Activity
제품 설명
IC50 & Target
[1]|
Cereblon 0.9 nM (Kd) |
IKZF1 |
IKZF3 |
In Vitro
Cemsidomide (0.3 nM; 1.5 h) promotes the degradation of >75% of IKZF1 in multiple myeloma cells. CFT7455 enables potent cell growth inhibition in both previously untreated NCIH929 multiple myeloma cell lines (IC50 of 0.071 nM) and NCIH929 cells made resistant to both Lenalidomide (HY-A0003)/Pomalidomide (HY-10984) (IC50 of 2.3 nM)[1].
Cemsidomide has potent antiproliferative activity against multiple myeloma cells and IMiD-resistant H929 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Cemsidomide (0.1 mg/kg/day; for 21 days) promotes tumor regression in the H929 tumor xenograft model (95% tumor growth inhibition by 7 days)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2504235-67-8
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Appearance Solid
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분자량 469.53
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화학식 C28H27N3O4
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Color Light yellow to green yellow
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SMILES
O=C1N([C@]2([H])C(NC(CC2)=O)=O)C3=CC=C(C4=CC=CC1=C43)CC5=CC=C(C=C5)CN6CCOCC6
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Synonyms
CFT7455
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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
In Vitro:
DMSO : 66.67 mg/mL (141.99 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 (5.32 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 (5.32 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.
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.
순도&문서
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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 | 2.1298 mL | 10.6489 mL | 21.2979 mL | 53.2447 mL |
| 5 mM | 0.4260 mL | 2.1298 mL | 4.2596 mL | 10.6489 mL | |
| 10 mM | 0.2130 mL | 1.0649 mL | 2.1298 mL | 5.3245 mL | |
| 15 mM | 0.1420 mL | 0.7099 mL | 1.4199 mL | 3.5496 mL | |
| 20 mM | 0.1065 mL | 0.5324 mL | 1.0649 mL | 2.6622 mL | |
| 25 mM | 0.0852 mL | 0.4260 mL | 0.8519 mL | 2.1298 mL | |
| 30 mM | 0.0710 mL | 0.3550 mL | 0.7099 mL | 1.7748 mL | |
| 40 mM | 0.0532 mL | 0.2662 mL | 0.5324 mL | 1.3311 mL | |
| 50 mM | 0.0426 mL | 0.2130 mL | 0.4260 mL | 1.0649 mL | |
| 60 mM | 0.0355 mL | 0.1775 mL | 0.3550 mL | 0.8874 mL | |
| 80 mM | 0.0266 mL | 0.1331 mL | 0.2662 mL | 0.6656 mL | |
| 100 mM | 0.0213 mL | 0.1065 mL | 0.2130 mL | 0.5324 mL |
Cemsidomide Related Classifications
HY-144841 Related Classifications
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