FHD-609
Based on 2 publication(s) in Google Scholar
FHD-609 is a BRD9 PROTAC degrader. FHD-609 induces BRD9 degradation, downregulates primary transcripts of HBG/HBD, Myc expression and proliferation gene sets, reduces the levels of synovial sarcoma tumor proliferation markers, and inhibits tumor growth. FHD-609 can be used in research related to advanced synovial sarcoma, SMARCB1-deficient tumors and adrenocortical carcinoma.
(Pink: BRD9 ligand (HY-49393); Blue: Cereblon ligand (HY-168308); Black: linker (HY-168309)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.95%
- CAS No.: 2676211-64-4
- Formule: C47H56N8O6
- Masse moléculaire:829.00
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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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Publications Citing Use of MedChemExpress (MCE) FHD-609
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Activité biologique
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BRD9 |
HBG |
HBD |
Acute treatment of primary human erythroid cultures with FHD-609 (10 nM; 2 h) directly reduces the ratio of HBD and HBG primary transcripts[1].
FHD-609 (5-500 nM; 4 h) dose-dependently reduces the relative mean fluorescence intensity of BRD9 in human peripheral blood mononuclear cells[4].
FHD-609 (0.5 μM; up to 8 h) has an epimerization half-life of 3.7 h in 0.1 M deuterated phosphate buffer at 37 °C, and it tends to adopt a linear conformation[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
FHD-609 (0.1-3 mg/kg; intravenous injection; single administration once every two weeks for a total of 5 times) induces rapid, dose-dependent degradation of BRD9 in PBMC immune cell subsets of CD-1 mice, and BRD9 levels gradually recover over time after the final administration[4].
FHD-609 (intravenous injection; single dose, once every two weeks for a total of 3 doses, once every two weeks for a total of 5 doses, dosage 0.1-3 mg/kg) dose-dependently reduces the expression level of MYC in SYO-1 CDX tumors, downregulates the Myc target gene set, and decreases proliferation markers (c-Myc, Ki67), while the expression levels of SSX-SS18 and TLE1 remain unchanged[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (immunodeficient; SYO-1 cell line-derived xenograft model)[4]
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Dosage:Potent antitumor activity (3.5 mg/kg; 0.7 mg/kg; 0.5 mg/kg)
Dose-dependent downregulation of MYC expression (0.1 mg/kg; 3 mg/kg) -
Administration:Potent antitumor activity (i.p.; weekly (3.5 mg/kg, 0.7 mg/kg); daily (0.5 mg/kg); 25 days)
Dose-dependent downregulation of MYC expression (i.v.; single dose, 3 biweekly doses, 5 biweekly doses) -
Result:Reduced tumor volume to <500 mm3 at 25 days post-treatment initiation (3.5 mg/kg i.p. weekly).
Reduced tumor volume to ~1000 mm3 at 25 days post-treatment initiation (0.7 mg/kg i.p. weekly).
Reduced tumor volume to <500 mm3 at 25 days post-treatment initiation (0.5 mg/kg i.p. daily).
Induced complete BRD9 degradation in tumor lysates collected 4 hours after the last dose (0.7 mg/kg or 3.5 mg/kg weekly).
Induced partial recovery of BRD9 levels in tumor lysates collected 7 days after the last dose (0.7 mg/kg or 3.5 mg/kg weekly).
Reduced MYC expression log2 fold-change relative to vehicle by -0.25 (0.1 mg/kg single dose), -0.73 (3 mg/kg single dose), -0.62 (0.1 mg/kg 3 doses), -1.02 (3 mg/kg 3 doses), -0.78 (0.1 mg/kg 5 doses), and -1.50 (3 mg/kg 5 doses), all with FDR-adjusted p-values ≤10-4.
Downregulated HALLMARK_MYC_TARGETS_V1 gene set with normalized enrichment scores (NES) ranging from -3.46 to -3.02 across all treatment groups.
Reduced c-Myc H-score to 143 (0.1 mg/kg 5 doses) and 102 (3 mg/kg 5 doses) compared to vehicle control H-score of 161.
Reduced Ki67 H-score to 148 (0.1 mg/kg 5 doses) and 118 (3 mg/kg 5 doses) compared to vehicle control H-score of 183.
Induced near-complete loss of BRD9 IHC staining in tumors treated with 3 mg/kg 5 doses.
Left SSX-SS18 and TLE1 staining unchanged relative to vehicle.
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Animal Model:CD-1 (immunocompetent; naïve)[4]
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Dosage:0.1 mg/kg; 3 mg/kg
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Administration:i.v.; single dose, 5 biweekly doses
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Result:Reduced relative BRD9 mean fluorescence intensity (MFI) normalized to vehicle to ~0 in B cells by 3 hours post-dose (0.1 mg/kg single dose), recovered to ~0.2 by 72 hours, and returned to vehicle levels by 504 hours.
Reduced relative BRD9 MFI normalized to vehicle to ~0 in B cells by 3 hours post-last dose (0.1 mg/kg 5 BIW doses), recovered to ~0.2 by 72 hours, and returned to vehicle levels by 504 hours.
Reduced relative BRD9 MFI normalized to vehicle to ~0 in B cells by 3 hours post-dose (3 mg/kg single dose), remained suppressed through 72 hours, and returned to vehicle levels by 504 hours.
Reduced relative BRD9 MFI normalized to vehicle to ~0 in B cells by 3 hours post-last dose (3 mg/kg 5 BIW doses), remained suppressed through 72 hours, was still ~0 at 168 hours post-last dose, and returned to vehicle levels by 504 hours.
Induced similar patterns of BRD9 degradation and recovery across B cells, CD4+ T cells, CD8+ T cells, monocytes, and NK cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2676211-64-4
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Appearance Solid
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Masse moléculaire 829.00
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Formule C47H56N8O6
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Color White to off-white
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SMILES
COC1=C(CN2CCC(CN3CCC4(CN(C5=CC(C(N([C@@H]6C(NC(CC6)=O)=O)C7)=O)=C7C=C5)C4)CC3)CC2)C(OC)=CC(C(C8=C9C=NC(N%10CCC%10)=C8)=CN(C)C9=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
Publications (2)
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Journal Impact Factor
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Most Recent
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Blood
Highly discriminative globin gene activation by the non-canonical BAF chromatin remodeling complex. [Abstract]2025 Nov 14:blood.2025029429. PMID: 41237357
FHD-609 purchased from MedChemExpress. Usage Cited in: Blood. 2025 Nov 14:blood.2025029429. [Abstract]
FHD-609 (10 nM; 2-4 h) degraded BRD9 in primary erythroid cultures.
FHD-609 purchased from MedChemExpress. Usage Cited in: Blood. 2025 Nov 14:blood.2025029429. [Abstract]
FHD-609 (10 nM; 2-4 h) decreased HBD and HBG primary transcripts in primary erythroid cells.
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Anal Chem
Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. [Abstract]2025 Dec 2;97(47):26097-26107. PMID: 41243541
Solvant et solubilité
DMSO : 100 mg/mL (120.63 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: ≥ 2.5 mg/mL (3.02 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.
Pureté et documentation
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Fiche technique (281 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
[1]. Bagchi A, et al. Highly discriminative globin gene activation by the noncanonical BAF chromatin remodeling complex. Blood. 2026 Feb 5;147(6):675-688. [Content Brief]
[2]. Livingston JA, et al. A Phase I Study of FHD-609, a Heterobifunctional Degrader of Bromodomain-Containing Protein 9, in Patients with Advanced Synovial Sarcoma or SMARCB1-Deficient Tumors. Clinical cancer research : an official journal of the American Association for Cancer Research. 2025 Feb 17;31(4):628-638. [Content Brief]
[5]. Yu ZJ, et al. Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. Analytical chemistry. 2025 Dec 02;97(47):26097-26107. [Content Brief]
[6]. Hescheler DA, et al. Targeted Therapy for Adrenocortical Carcinoma: A Genomic-Based Search for Available and Emerging Options. Cancers. 2022 May 31;14(11):2721. [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 |
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| DMSO | 1 mM | 1.2063 mL | 6.0314 mL | 12.0627 mL | 30.1568 mL |
| 5 mM | 0.2413 mL | 1.2063 mL | 2.4125 mL | 6.0314 mL | |
| 10 mM | 0.1206 mL | 0.6031 mL | 1.2063 mL | 3.0157 mL | |
| 15 mM | 0.0804 mL | 0.4021 mL | 0.8042 mL | 2.0105 mL | |
| 20 mM | 0.0603 mL | 0.3016 mL | 0.6031 mL | 1.5078 mL | |
| 25 mM | 0.0483 mL | 0.2413 mL | 0.4825 mL | 1.2063 mL | |
| 30 mM | 0.0402 mL | 0.2010 mL | 0.4021 mL | 1.0052 mL | |
| 40 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7539 mL | |
| 50 mM | 0.0241 mL | 0.1206 mL | 0.2413 mL | 0.6031 mL | |
| 60 mM | 0.0201 mL | 0.1005 mL | 0.2010 mL | 0.5026 mL | |
| 80 mM | 0.0151 mL | 0.0754 mL | 0.1508 mL | 0.3770 mL | |
| 100 mM | 0.0121 mL | 0.0603 mL | 0.1206 mL | 0.3016 mL |
FHD-609 Related Classifications
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