Art. -Nr.: HY-145925B

CFT8634

Name: CFT8634
Brand: MedChemExpress
SKU: HY-145925B
Price: 328.00 USD
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3 Cited Publications

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CFT8634 is an orally active BRD9 PROTAC degrader with a DC₅₀ of 0.003 μM (HEK293T.166). CFT8634 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, triggering CRBN-catalyzed BRD9 polyubiquitination and 26S proteasome-mediated degradation. CFT8634 induces sustained tumor regression and inhibits tumor growth in mouse models. CFT8634 can be used in research related to synovial sarcoma, SMARCB-1-deficient cancers, acute myeloid leukemia, malignant rhabdoid tumors, and multiple myeloma.
(Pink: BRD9 ligand (HY-169988); Blue: Cereblon ligand (HY-169989); Black: linker (HY-169991)).

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Reinheit : 98.10%
CAS. Nr.: 2704617-96-7
Formel: C₃₇H₄₅F₃N₆O₅
Molecular Weight:710.79

Speicherung:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

CFT8634 Chemical Structure

CAS. Nr.: 2704617-96-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CFT8634 is an orally active BRD9 PROTAC degrader with a DC₅₀ of 0.003 μM (HEK293T.166). CFT8634 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, triggering CRBN-catalyzed BRD9 polyubiquitination and 26S proteasome-mediated degradation. CFT8634 induces sustained tumor regression and inhibits tumor growth in mouse models. CFT8634 can be used in research related to synovial sarcoma, SMARCB-1-deficient cancers, acute myeloid leukemia, malignant rhabdoid tumors, and multiple myeloma^[1]^[2]^[3]. (Pink: BRD9 ligand (HY-169988); Blue: Cereblon ligand (HY-169989); Black: linker (HY-169991)).

IC₅₀ & Target

^[1]

BRD9

0.003 μM (DC₅₀)

Cereblon

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In Vitro

CFT8634 potently and selectively degrades BRD9 in synovial sarcoma and SMARCB-1-deficient cells, with a DC₅₀ of 2.7 nM^[1].
CFT8634 (10 μM; 2 h) potently degrades BRD9 in HEK293T.166 cells, with a DC₅₀ of 0.003 μM and an E_max of 4%^[2].
CFT8634 (100 nM; 4 h) selectively degrades BRD9 in HSSYII human synovial sarcoma cells^[2].
The degradation of BRD9 induced by CFT8634 (1 μM; 4 h) in Yamato-SS cells depends on the ubiquitin-proteasome system, BRD9 binding, and CRBN binding^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[2]

Cell Line:

Yamato-SS human synovial sarcoma cells
Concentration:

1 μM (CFT8634); 10 μM (competitor agents: Bortezomib (HY-10227), MLN-4924 (HY-70062), BI-7273 (HY-100351), CRBN binder)
Incubation Time:

4 h (CFT8634 incubation); 1 h (competitor pre-incubation) followed by 4 h (co-incubation with CFT8634)
Result:

Induced BRD9 degradation that was rescued by co-treatment with bortezomib, BI-7273, MLN-4924, or a CRBN binder.
Did not reduce BRD9 levels when competitors were used alone.

Parmacokinetics

Species	Dose	Route	CL	T_1/2	V_dss	Bioavailability
Mice^[2]	2 mg/kg	i.v.	6.2 mL/min/kg	3.7 h	2.0 L/kg	/
Mice^[2]	10 mg/kg	p.o.	/	3.5 h	/	74 %
Rat^[2]	1 mg/kg	i.v.	16.6 mL/min/kg	3.9 h	4.0 L/kg	/
Rat^[2]	10 mg/kg	p.o.	/	5.4 h	/	97 %
Dog^[2]	1 mg/kg	i.v.	4.7 mL/min/kg	10.2 h	2.2 L/kg	/
Dog^[2]	1 mg/kg	p.o.	/	9.8 h	/	86 %

In Vivo

CFT8634 (0.3-50 mg/kg; p.o.; once daily; for 21 consecutive days) induces dose-dependent BRD9 degradation in Yamato-SS synovial sarcoma xenografts, with a maximum tumor growth inhibition rate of up to 92%^[2].
CFT8634 (0.01-30 mg/kg; p.o.; once daily; for 21 consecutive days) induces dose-dependent BRD9 degradation in SA13412 synovial sarcoma xenografts, achieving up to 100% tumor growth inhibition^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (female, 6-8 weeks old, 18-22 g, subcutaneous inoculation of Yamato-SS cells)^[2]
Dosage:

0.3-50 mg/kg (daily dosing for 21 days); 0.3-50 mg/kg (single dose)
Administration:

p.o.; daily; 21 days; p.o.; single dose
Result:

Achieved ≥90% BRD9 degradation in tumors by 4 hours at doses ≥1 mg/kg.
Maintained maximal BRD9 degradation for 24 hours at 30 and 50 mg/kg single doses.
Produced dose-dependent tumor growth inhibition (TGI): 31% at 0.3 mg/kg, 92% at 50 mg/kg.
Caused only mild weight loss at the three highest doses, with overall good tolerance.

Animal Model:

NOD/SCID nude (female, 6-9 weeks old, subcutaneous implantation of SA13412 patient-derived tumor fragments)^[2]
Dosage:

0.01-30 mg/kg (daily dosing for 21 days); 0.01-30 mg/kg (single dose)
Administration:

p.o.; daily; 21 days; p.o.; single dose
Result:

Achieved ~90% BRD9 degradation in tumors by 4 hours at 1 and 30 mg/kg single doses.
Maintained maximal BRD9 degradation for 24 hours at 30 mg/kg single dose.
Produced dose-dependent tumor growth inhibition (TGI): 72% at 0.1 mg/kg, 95% at 1 mg/kg, 100% at 30 mg/kg.
Was well-tolerated across all doses tested.

Clinical Trial

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

Chemical Information

CAS. Nr. 2704617-96-7
Appearance Solid
Molecular Weight 710.79
Formel C₃₇H₄₅F₃N₆O₅
Color Light green to gray
SMILES

CC(C(C1=CC(OC)=C(C(OC)=C1)CN2CC(F)([C@@H](N3CCN(C4=C(C=C(C=C4)N[C@@H]5C(NC(CC5)=O)=O)F)CC3)CC2)F)=CN6C)=C(C)C6=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Publications (3)

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Drug Metab Dispos

2026 Jul 17.
Drug Metab Dispos

2026 Jul 14;54(8):100365. PMID: 42561496
University of Toronto

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (140.69 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

1.4069 mL

7.0344 mL

14.0689 mL

5 mM

0.2814 mL

1.4069 mL

2.8138 mL

10 mM

0.1407 mL

0.7034 mL

1.4069 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 (protect from light, stored under nitrogen). 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.52 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.52 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 3

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

Solubility: ≥ 2.5 mg/mL (3.52 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 (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Zeng S, et al. Current advances and development strategies of orally bioavailable PROTACs. European journal of medicinal chemistry. 2023 Dec 05;261:115793. [Content Brief]

[2]. Jackson KL, et al. Discovery of CFT8634, a Potent, Selective, and Orally Bioavailable Heterobifunctional Degrader of BRD9. Journal of medicinal chemistry. 2025 Dec 11;68(23):24848-24868. [Content Brief]

[3]. Christopher G. Nasveschuk, et al. Compounds for targeted degradation of brd9. WO2021178920A1. 2022-09-05.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4069 mL	7.0344 mL	14.0689 mL	35.1721 mL
	5 mM	0.2814 mL	1.4069 mL	2.8138 mL	7.0344 mL
	10 mM	0.1407 mL	0.7034 mL	1.4069 mL	3.5172 mL
	15 mM	0.0938 mL	0.4690 mL	0.9379 mL	2.3448 mL
	20 mM	0.0703 mL	0.3517 mL	0.7034 mL	1.7586 mL
	25 mM	0.0563 mL	0.2814 mL	0.5628 mL	1.4069 mL
	30 mM	0.0469 mL	0.2345 mL	0.4690 mL	1.1724 mL
	40 mM	0.0352 mL	0.1759 mL	0.3517 mL	0.8793 mL
	50 mM	0.0281 mL	0.1407 mL	0.2814 mL	0.7034 mL
	60 mM	0.0234 mL	0.1172 mL	0.2345 mL	0.5862 mL
	80 mM	0.0176 mL	0.0879 mL	0.1759 mL	0.4397 mL
	100 mM	0.0141 mL	0.0703 mL	0.1407 mL	0.3517 mL

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Keywords

CFT8634

3 Cited Publications

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CFT8634

Publications Citing Use of MedChemExpress (MCE) CFT8634

Alle PROTACs Isoform-spezifische Produkte anzeigen

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