Art. -Nr.: HY-181854

ZX079

ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC₅₀ value of 0.035 nM and a CBP DC₅₀ value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia.
(Pink: ligand (HY-181759); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W105740)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3124583-65-6
Formel: C₄₇H₅₆F₃N₇O₇
Molecular Weight:887.99

Speicherung:

-20°C, protect from light

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

ZX079 Chemical Structure

CAS. Nr.: 3124583-65-6

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Preis

Verfügbarkeit

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC₅₀ value of 0.035 nM and a CBP DC₅₀ value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia^[1]. (Pink: ligand (HY-181759); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W105740)).

IC₅₀ & Target

^[1]

BRD4

0.035 nM (DC₅₀)

BRD4(1)

0.9 μM (IC₅₀)

BRD4(2)

0.5 μM (IC₅₀)

CBP

p300

Caspase 3

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

In Vitro

ZX079 (10k) (24 h) exhibits dose- and time-dependent degradation of BRD4 (DC₅₀ = 0.035 nM), CBP, p300 and BRD3 (DC₅₀ < 0.02 nM) without significant degradation of BRD2^[1].
ZX079 (0.0001-100 μM) binds potently to BRD4 (1) (IC₅₀ = 0.9 μM), BRD4 (2) (IC₅₀ = 0.5 μM), and CBP bromodomains (IC₅₀ = 1.2 μM) and effectively promotes BRD4-PROTAC-CRBN and CBP-PROTAC-CRBN ternary complex assembly^[1].
ZX079 (0.02-200 nM; 96 h) exerts superior antiproliferative activity against MV4-11 cells (IC₅₀ = 0.86 nM) and MOLM-13 cells, while it shows minimal cytotoxicity against normal HUVEC and L929 cells (tested at 0.001-10 μM)^[1].
ZX079 (200 nM; 8 h) selectively depletes BRD4, BRD3, CBP, and p300 proteins in MV4-11 cells at the proteome-wide level.
ZX079 (37-1000 nM; 48 h) induces apoptosis in MV4-11 and MOLM-13 cells in a dose-dependent manner, accompanied by increased cleavage of Caspase-3 and almost complete reduction of c-Myc protein expression at 2 nM^[1].

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

Cell Viability Assay^[1]

Cell Line:

MV4-11 and MOLM-13 acute myeloid leukemia cells, HUVEC, L929 normal cells
Concentration:

10^-6, 10^-4, 10^-2, 10⁰, 10² μM (MV4-11 and MOLM-13 cells); 0.01, 0.01, 0.1, 1, 10, 100 μM (HUVEC and L929 cells)
Incubation Time:

96 h (MV4-11 and MOLM-13 cells); 48 h (HUVEC and L929 cells)
Result:

Exhibited an IC₅₀ of 0.86 nM in MV4-11 cells and 18.93 nM in MOLM-13 cells.
Exhibited minimal cytotoxicity toward HUVEC and L929 cells.

Western Blot Analysis^[1]

Cell Line:

MV4-11 acute myeloid leukemia cells
Concentration:

0.02, 0.2, 2.0, 20, 200 nM (24 h); 200 nM (time-course); 2 nM, 200 nM (24 h)
Incubation Time:

1 h, 2 h, 4 h, 8 h, 12 h, 24 h (time-course); 24 h (fixed time)
Result:

Achieved 95% degradation of BRD4 and 74% degradation of CBP at 2 nM after 24 h.
Achieved 98% degradation of BRD4 and 99% degradation of CBP at 200 nM after 24 h.
Induced rapid degradation of CBP within 2 h, with near-complete depletion by 4 h.
Reduced BRD4 levels in a time-dependent manner over 24 h.
Exhibited a DC₅₀ of 0.035 nM for BRD4, < 0.02 nM for CBP, and < 0.02 nM each for p300 and BRD3.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 and MOLM-13 acute myeloid leukemia cells
Concentration:

37, 111, 333, 1000 nM
Incubation Time:

48 h
Result:

Potently induced apoptosis in a dose-dependent manner, achieving over 60% apoptosis at 37 nM in MV4-11 cells.
Led to markedly increased cleaved caspase-3 levels and almost completely reduced c-Myc protein expression in MV4-11 cells at 20 nM.
Induced dose-dependent apoptosis in MOLM-13 cells.

Parmacokinetics

Species	Dose	Route	AUC_last	C_max	CL	T_1/2	F
Rat^[1]	10 mg/kg	p.o.	43.9 μg/L·h	9.5 μg/L	- L/h/kg	2.13 h	1.48 %
Rat^[1]	2 mg/kg	i.v.	610 μg/L·h	634 μg/L	3.28 L/h/kg	1.74 h	/

In Vivo

ZX079 (10k) (2-10 mg/kg; intraperitoneal injection; twice weekly/weekly; 21 days) exhibits potent in vivo antitumor activity in an AML xenograft model, achieving 91-93% tumor growth inhibition with two distinct intraperitoneal dosing regimens, while maintaining tolerability^[1].

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

Animal Model:

NOD SCID (female, 4 weeks old, subcutaneous xenograft model)^[1]
Dosage:

2 mg/kg (twice weekly); 10 mg/kg (weekly)
Administration:

intraperitoneal injection; 21 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 93% with 2 mg/kg twice-weekly dose.
Achieved a TGI rate of 91% with 10 mg/kg weekly dose.
Caused no significant body weight loss compared to vehicle control.
Induced degradation of BRD4 and CBP proteins in harvested tumors.
Significantly reduced c-Myc protein expression relative to vehicle control.

Related Protocols :

Chemical Information

CAS. Nr. 3124583-65-6
Appearance Solid
Molecular Weight 887.99
Formel C₄₇H₅₆F₃N₇O₇
Color Light yellow to green yellow
SMILES

O=C(NC(CC1)=O)C1N(C2=O)C(C(C2=C3)=CC=C3NCCCCCCCCCCCC(N(CC4)CCC4C5=NC6=CC=C(C(C=C7C)=CN(C)C7=O)C=C6N5CCOC(F)(F)F)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (112.61 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

1.1261 mL

5.6307 mL

11.2614 mL

5 mM

0.2252 mL

1.1261 mL

2.2523 mL

10 mM

0.1126 mL

0.5631 mL

1.1261 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). 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 (2.82 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 (2.82 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.

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]. Xiang Q, et al. Discovery of ZX079 as a Dual PROTAC Degrader Targeting BRD4/CBP in Acute Myeloid Leukemia. J Med Chem. 2026;69(4):4132-4159. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1261 mL	5.6307 mL	11.2614 mL	28.1535 mL
	5 mM	0.2252 mL	1.1261 mL	2.2523 mL	5.6307 mL
	10 mM	0.1126 mL	0.5631 mL	1.1261 mL	2.8153 mL
	15 mM	0.0751 mL	0.3754 mL	0.7508 mL	1.8769 mL
	20 mM	0.0563 mL	0.2815 mL	0.5631 mL	1.4077 mL
	25 mM	0.0450 mL	0.2252 mL	0.4505 mL	1.1261 mL
	30 mM	0.0375 mL	0.1877 mL	0.3754 mL	0.9384 mL
	40 mM	0.0282 mL	0.1408 mL	0.2815 mL	0.7038 mL
	50 mM	0.0225 mL	0.1126 mL	0.2252 mL	0.5631 mL
	60 mM	0.0188 mL	0.0938 mL	0.1877 mL	0.4692 mL
	80 mM	0.0141 mL	0.0704 mL	0.1408 mL	0.3519 mL
	100 mM	0.0113 mL	0.0563 mL	0.1126 mL	0.2815 mL

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ZX079

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen