Art. -Nr.: HY-153367

FHD-609

2 Cited Publications

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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)).

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Reinheit: 98.95%
CAS. Nr.: 2676211-64-4
Formel: C₄₇H₅₆N₈O₆
Molecular Weight:829.00

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

FHD-609 Chemical Structure

CAS. Nr.: 2676211-64-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]^[2]^[3]^[4]^[5]^[6]. (Pink: BRD9 ligand (HY-49393); Blue: Cereblon ligand (HY-168308); Black: linker (HY-168309)).

IC₅₀ & Target^[1]^[3]^[4]

BRD9

HBG

HBD

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

In Vitro

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.

In Vivo

FHD-609 (i.p.; administered weekly/daily; for a duration of 25 days at doses of 0.5-3.5 mg/kg) exerts dose-dependent tumor growth inhibition in the SYO-1 CDX model of synovial sarcoma^[4].
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.

Animal Model:

BALB/c nude (immunodeficient; SYO-1 cell line-derived xenograft model)^[4]
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.

Animal Model:

CD-1 (immunocompetent; naïve)^[4]
Dosage:

0.1 mg/kg; 3 mg/kg
Administration:

i.v.; single dose, 5 biweekly doses
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2676211-64-4
Appearance Solid
Molecular Weight 829.00
Formel C₄₇H₅₆N₈O₆
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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.
Anal Chem

Hydrogen/Deuterium Exchange for Chiral Stability Assessment in Acidic Methine-Containing Compounds. [Abstract]

2025 Dec 2;97(47):26097-26107. PMID: 41243541

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2063 mL

6.0314 mL

12.0627 mL

5 mM

0.2413 mL

1.2063 mL

2.4125 mL

10 mM

0.1206 mL

0.6031 mL

1.2063 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

[3]. Lin M, Adam A, et al. Long acting injectable FHD-609 micro-suspension: A potent BRD9 degrader with comparable efficacy, reduced frequency of dosing in preclinical models[C]//Cancer Research. 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH, 2024, 84(6).

[4]. Collins M, et al. Preclinical validation of target engagement assays and investigation of mechanistic impacts of FHD-609, a clinical-stage BRD9 degrader being developed for the treatment of synovial sarcoma[J]. strategies, 2022, 36: 936-950.

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.2063 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

2 Cited Publications

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FHD-609

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Publications Citing Use of MedChemExpress (MCE) FHD-609

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FHD-609

Apoptosis Compound Library

Epigenetics Compound Library

Metabolism/Protease Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Reprogramming Compound Library

Endocrinology Compound Library

Glutamine Metabolism Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Mitochondrial Protection Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Clinical Compound Library Plus

Bioactive Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) FHD-609

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FHD-609 Related Classifications

HY-153367 Related Classifications