Camibirstat
Based on 3 publication(s) in Google Scholar
FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.79%
- No. CAS: 2671128-05-3
- Fòrmula: C24H30N6O6S2
- Peso molecular:562.66
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Almacenamiento: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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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) Camibirstat
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Customer Validation & Images
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Cell Imaging/Staining
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IF
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Flow Cytometry
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
Ver todos los productos específicos de isoformas SWI/SNF Complex
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Actividad biológica
FHD-286 (10 to 100 nM) for 7 days induces differentiation followed by loss of viability of AML cell lines and PD AML cells with MLL rearrangement (r), mutant (mt) NPM1 and chromosome 3q26 lesions (with EVI1 overexpression). Treatment with FHD-286 causes whole-genome, concordant, up- or down-regulations in ATAC-Seq peaks and RNA-Seq-determined mRNA expressions of specific loci, associated with significant reduction in the gene-sets of targets of MYC, mTORC1, E2F, Interferon-gamma, IL6-JAK-STAT3, as well as of inflammatory response and oxidative phosphorylation genes. QPCR analyses determined significant reduction in mRNA expression of MYC, SPI1 and BCL2 genes. Mass spectrometry on AML cell lysates treated with FHD-286 showed log2 fold-reductions in c-Myc, SPI1, MEF2C, KMT2C and CDK4 (in MOLM13) and in EVI1, c-Myb, CDK6 and c-Myc (in AML191) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B16F10 tumor-bearing mice[2]
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Dosage:1.5 mg/kg
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Administration:Oral administration; for 10 days
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Result:Increased in IFNγ and Th1-type chemokine CXCL10 levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2671128-05-3
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Appearance Solid
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Peso molecular 562.66
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Fòrmula C24H30N6O6S2
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Color Off-white to light yellow
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SMILES
COC[C@@H](C(NC1=NC(C2=CC=CC(N3C[C@@H](O[C@@H](C3)C)C)=N2)=CS1)=O)NC(C4=CN(C=C4)S(C)(=O)=O)=O
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Synonyms
FHD-286
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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 (3)
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Journal Impact Factor
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Most Recent
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Mol Cell
2025 Aug 21;85(16):3041-3056.e9. PMID: 40695292 -
bioRxiv
Spatially-Resolved Multiomic Atlas of Leiomyosarcoma Identifies Two Clinically Relevant Epigenetically-Driven Cell States. [Abstract]2026 May 26:2026.05.22.726988. PMID: 42244620 -
Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.
HeLa cells were pre-treated with or without 1 μM FHD286 for two hours. Laser microirradiation was performed to examine the localization of SMARCA2, SMARCC1 and SMARCD1.
Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.
Lacking the enzymatic activities of SMARCA2/4 extends the accumulation of γH2AX, RNF8 and BRCA1. HeLa cells were pre-treated with or without FHD286 (1 μM) or Compound 14 (1 μM) for two hours followed by 5 Gy of IR. Following the indicated recovery time, the foci of γH2AX, RNF8 and BRCA1 were examined by IF.
Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.
HR efficacy was examined by GFP reporter assays. U2OS cells with DR-GFP insertion were pretreated with or without FHD286 (1 μM) or Compound 14 (1 μM). I-SceI were expressed to induce DSBs. GFP positive populations were calculated by flowcytometry.
Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.
1000 cells were seeded in each well, and treated with indicated doses of FHD286 and/or olaparib. Colony formation was examined at Day 14 with 0.1% crystal violet staining. Statistical analyses were shown in the lower panel.
Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.
HeLa cells were pre-treated with or without FHD286 (1 μM) or Compound 14 (1 μM) for two hours followed by 5 Gy of IR. Foci formation of RAD51, SMARCA2 were examined.
Solvente y solubilidad
DMSO : 250 mg/mL (444.32 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 1.7773 mL | 8.8864 mL | 17.7727 mL | 44.4318 mL |
| 5 mM | 0.3555 mL | 1.7773 mL | 3.5545 mL | 8.8864 mL | |
| 10 mM | 0.1777 mL | 0.8886 mL | 1.7773 mL | 4.4432 mL | |
| 15 mM | 0.1185 mL | 0.5924 mL | 1.1848 mL | 2.9621 mL | |
| 20 mM | 0.0889 mL | 0.4443 mL | 0.8886 mL | 2.2216 mL | |
| 25 mM | 0.0711 mL | 0.3555 mL | 0.7109 mL | 1.7773 mL | |
| 30 mM | 0.0592 mL | 0.2962 mL | 0.5924 mL | 1.4811 mL | |
| 40 mM | 0.0444 mL | 0.2222 mL | 0.4443 mL | 1.1108 mL | |
| 50 mM | 0.0355 mL | 0.1777 mL | 0.3555 mL | 0.8886 mL | |
| 60 mM | 0.0296 mL | 0.1481 mL | 0.2962 mL | 0.7405 mL | |
| 80 mM | 0.0222 mL | 0.1111 mL | 0.2222 mL | 0.5554 mL | |
| 100 mM | 0.0178 mL | 0.0889 mL | 0.1777 mL | 0.4443 mL |
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