Safusidenib
Based on 2 publication(s) in Google Scholar
Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
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- Pureza: 99.05%
- No. CAS: 1898206-17-1
- Fòrmula: C25H18Cl3FN2O4
- Peso molecular:535.78
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Almacenamiento:Powder -20°C, 3 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
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Safusidenib
More
Actividad biológica
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IDH1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| TF-1 | IC50 |
29 nM
Compound: 93; DS1001b
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Anticancer activity against human TF-1 cells assessed as cell growth inhibition
Anticancer activity against human TF-1 cells assessed as cell growth inhibition
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[PMID: 37235998] |
Safusidenib (DS-1001b) impairs the proliferation of IDH1-mutated chondrosarcoma cell lines and decreases 2-HG levels[1].
Safusidenib impairs the proliferation of IDH1 mutant chondrosarcoma cell lines in a dose-dependent manner, whereas Safusidenib has little effect on the proliferation of the IDH wild-type cell lines OUMS27 and NDCS-1; GI50 values for JJ012, L835, OUMS27, and NDCS-1 cells are 81?nM (day 14), 77?nM (6 weeks), >10?μM (day 10), and >10?μM (day 10), respectively[1].
Safusidenib (1, and 10?μM; for 6 weeks) markedly upregulates SOX9, a key regulator of chondrocyte differentiation, at the protein level[1].
Safusidenib (1 μM) significantly upregulates CDKN1C at the protein level[1].
Safusidenib (DS-1001b) exhibits activity against IDH1 or IDH2 enzymes with IC50s of 8.4, 11, and 180 nM for IDH1R132H, IDH1R132C, and IDH1WT in assays conducted with a 2-hour preincubation step[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:The IDH1 mutant cell lines JJ012 and L835 cells
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Concentration:0.1, 1, and 10 μM
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Incubation Time:0, 3, 6, 9, 12, and 15 days
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Result:Impaired proliferation in both cell lines in a dose-dependent manner.
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Cell Line:L835 cells
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Concentration:0, 1, and 10 μM
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Incubation Time:6 weeks
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Result:Markedly upregulated SOX9 at the protein level.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID bearing JJ012 xenograft[3]
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Dosage:Mixed with sterilized pellet food (CRF-1; Oriental Yeast) and fed ad libitum for 6 weeks. Mixed with sterilized pellet food (CRF-1; Oriental Yeast) and fed ad libitum for 6 weeks.
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Administration:Fed continuously starting at 3 weeks
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Result:Continuous administration significantly impaired tumor growth in JJ012 xenograft mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1898206-17-1
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Appearance Solid
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Peso molecular 535.78
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Fòrmula C25H18Cl3FN2O4
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Color Light yellow to yellow
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SMILES
O=C(N1C2=CC=CC(/C=C/C(O)=O)=C2C(C)=C1)C3=C(C(C)(F)C)ON=C3C4=C(C=C(C=C4Cl)Cl)Cl
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Synonyms
AB-291; DS-1001
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Resistance to the isocitrate dehydrogenase 1 mutant inhibitor ivosidenib can be overcome by alternative dimer-interface binding inhibitors. [Abstract]2022 Aug 15;13(1):4785. PMID: 35970853 -
Nat Chem Biol
2026 Jan 13. PMID: 41530531
Solvente y solubilidad
DMSO : 100 mg/mL (186.64 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 (4.67 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 (283 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
[1]. Makoto Nakagawa, et al. Selective inhibition of mutant IDH1 by DS-1001b ameliorates aberrant histone modifications and impairs tumor activity in chondrosarcoma. Oncogene. 2019 Oct;38(42):6835-6849. [Content Brief]
[2]. Yukino Machida, et al. A Potent Blood-Brain Barrier-Permeable Mutant IDH1 Inhibitor Suppresses the Growth of Glioblastoma with IDH1 Mutation in a Patient-Derived Orthotopic Xenograft Model. Mol Cancer Ther. 2020 Feb;19(2):375-383. [Content Brief]
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 | 1.8664 mL | 9.3322 mL | 18.6644 mL | 46.6609 mL |
| 5 mM | 0.3733 mL | 1.8664 mL | 3.7329 mL | 9.3322 mL | |
| 10 mM | 0.1866 mL | 0.9332 mL | 1.8664 mL | 4.6661 mL | |
| 15 mM | 0.1244 mL | 0.6221 mL | 1.2443 mL | 3.1107 mL | |
| 20 mM | 0.0933 mL | 0.4666 mL | 0.9332 mL | 2.3330 mL | |
| 25 mM | 0.0747 mL | 0.3733 mL | 0.7466 mL | 1.8664 mL | |
| 30 mM | 0.0622 mL | 0.3111 mL | 0.6221 mL | 1.5554 mL | |
| 40 mM | 0.0467 mL | 0.2333 mL | 0.4666 mL | 1.1665 mL | |
| 50 mM | 0.0373 mL | 0.1866 mL | 0.3733 mL | 0.9332 mL | |
| 60 mM | 0.0311 mL | 0.1555 mL | 0.3111 mL | 0.7777 mL | |
| 80 mM | 0.0233 mL | 0.1167 mL | 0.2333 mL | 0.5833 mL | |
| 100 mM | 0.0187 mL | 0.0933 mL | 0.1866 mL | 0.4666 mL |
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