Felezonexor
Based on 1 Customer Validation
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells.
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- Purity: 99.79%
- CAS No.: 1076235-04-5
- 화학식: C18H21ClF3N3O3
- 분자량:419.83
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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
Biological Activity
CRM1[1]
CBS9106 (0.01-10 μM; 72 hours) sensitizes cells to radiation and to suppress the growth of a variety of cancer cell lines. The estimated IC50 values range from 22.3 or 35.6 nM in multiple myeloma (MM).1S or RPMI-8226 cells and from 3 to 278 nM in 60 other human cancer cell lines[1].
CBS9106 (1-400 nM; 24 hours) decreases CRM1 protein expression levels in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S cells, RPMI-8226 cells
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Concentration:0.01, 0.1, 10 μM
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Incubation Time:72 hours
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Result:Suppressed the growth of a variety of cancer cell lines and the estimated IC50 values ranged from 22.3 or 35.6 nM in MM.1S or RPMI-8226 cells.
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Cell Line:MM.1S cells
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Concentration:1, 3, 6, 12, 25, 50, 100, 200, 400 nM
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Incubation Time:24 hours
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Result:The level of CRM1 protein expression markedly reduced in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice with RPMI-8226 cells[1]
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Dosage:31.25, 62.5, 125 mg/kg
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Administration:Oal administration; 5 times weekly (31.25 and 62.5 mg/kg), 3 times weekly (125 mg/kg); 2 weeks
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Result:Showed statistically significant tumor growth inhibition at dose levels of 62.5 mg/kg or 125 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1076235-04-5
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Appearance Solid
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분자량 419.83
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화학식 C18H21ClF3N3O3
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Color White to off-white
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SMILES
O=C(C(COCCC(C)(C)C)=C1C)N(NC2=NC(Cl)=C(C(F)(F)F)C=C2)C1=O
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Synonyms
CBS9106; SL-801
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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 (238.19 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 (5.95 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 (5.95 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 (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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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 | 2.3819 mL | 11.9096 mL | 23.8192 mL | 59.5479 mL |
| 5 mM | 0.4764 mL | 2.3819 mL | 4.7638 mL | 11.9096 mL | |
| 10 mM | 0.2382 mL | 1.1910 mL | 2.3819 mL | 5.9548 mL | |
| 15 mM | 0.1588 mL | 0.7940 mL | 1.5879 mL | 3.9699 mL | |
| 20 mM | 0.1191 mL | 0.5955 mL | 1.1910 mL | 2.9774 mL | |
| 25 mM | 0.0953 mL | 0.4764 mL | 0.9528 mL | 2.3819 mL | |
| 30 mM | 0.0794 mL | 0.3970 mL | 0.7940 mL | 1.9849 mL | |
| 40 mM | 0.0595 mL | 0.2977 mL | 0.5955 mL | 1.4887 mL | |
| 50 mM | 0.0476 mL | 0.2382 mL | 0.4764 mL | 1.1910 mL | |
| 60 mM | 0.0397 mL | 0.1985 mL | 0.3970 mL | 0.9925 mL | |
| 80 mM | 0.0298 mL | 0.1489 mL | 0.2977 mL | 0.7443 mL | |
| 100 mM | 0.0238 mL | 0.1191 mL | 0.2382 mL | 0.5955 mL |
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