Cat. No.: HY-182912

PLX-4104

PLX-4104 is an orally active BRD4 molecular glue degrader with a DC₅₀ of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia.

For research use only. We do not sell to patients.

CAS No.: 2851986-77-9
Formula: C₃₂H₂₆FN₉O₂S
Molecular Weight:619.67

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PLX-4104 Chemical Structure

CAS No.: 2851986-77-9

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

BRD4

2 nM (DC₅₀)

DCAF11

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In Vitro

PLX-4104 potently binds to BRD4 with an IC₅₀ of 4 nM^[1].
PLX-4104 (24 h) induces near-complete (>95%) BRD4 degradation in MV-4-11 cells with a DC₅₀ of 2 nM^[1].
PLX-4104 (72 h) potently inhibits the proliferation of MV-4-11 cells with an EC₅₀ of 4 nM^[1].
PLX-4104 has intrinsic clearance of 11.1 mL/min/kg in human liver microsomes and <10 mL/min/kg in mouse liver microsomes^[1].

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

Parmacokinetics

Species	Dose	Route	CL	T_1/2	V_ss	AUC_0-inf	C_max	T_max	F
Mice^[1]	1 mg/kg	i.v.	16.6 mL/min/kg	1.2 h	1.1 L/kg	/	/	/	/
Mice^[1]	50 mg/kg	p.o.	/	/	/	19.0 μM·h	6.74 μM	2.0 h	23 %
Rat^[1]	1 mg/kg	i.v.	8.1 mL/min/kg	1.1 h	0.6 L/kg	/	/	/	/
Rat^[1]	10 mg/kg	p.o.	/	/	/	3.7 μM·h	0.87 μM	2.0 h	11 %
Dog^[1]	1 mg/kg	i.v.	2.5 mL/min/kg	2.8 h	0.5 L/kg	/	/	/	/
Dog^[1]	5 mg/kg	p.o.	/	/	/	8.0 μM·h	1.49 μM	1.7 h	14 %

In Vivo

PLX-4104 (2-6 mg/kg; p.o.; daily; 21 days) elicits dose-dependent antitumor efficacy in AML MV-4-11 xenografts without significant body weight changes^[1].

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

Animal Model:

NOD-SCID mice with AML MV-4-11 xenografts^[1]
Dosage:

2 mg/kg; 6 mg/kg
Administration:

p.o.; daily; 21 days
Result:

Achieved approximately 50% tumor growth inhibition (TGI) by day 21 (2 mg/kg).
Achieved complete tumor regression, with no measurable tumors detected on day 21 (6 mg/kg).
Caused no significant changes in mouse body weight with either dose.

Chemical Information

CAS No. 2851986-77-9
Molecular Weight 619.67
Formula C₃₂H₂₆FN₉O₂S
SMILES

O=C(NC1=C(F)C=CC(C2=CC=C(C3=N[C@@H](CC(N)=O)C4=NN=C(C)N4C5=C3C(C)=C(C)S5)C=C2)=C1)C6=C7N=CC=CN7N=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (161.38 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

1.6138 mL

8.0688 mL

16.1376 mL

5 mM

0.3228 mL

1.6138 mL

3.2275 mL

10 mM

0.1614 mL

0.8069 mL

1.6138 mL

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (4.03 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 (4.03 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 (4.03 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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Leriche G, et al. Discovery and Structural Optimization of BRD4-Selective Monovalent Direct Degraders[J]. ACS Medicinal Chemistry Letters, 2026.

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	1.6138 mL	8.0688 mL	16.1376 mL	40.3441 mL
	5 mM	0.3228 mL	1.6138 mL	3.2275 mL	8.0688 mL
	10 mM	0.1614 mL	0.8069 mL	1.6138 mL	4.0344 mL
	15 mM	0.1076 mL	0.5379 mL	1.0758 mL	2.6896 mL
	20 mM	0.0807 mL	0.4034 mL	0.8069 mL	2.0172 mL
	25 mM	0.0646 mL	0.3228 mL	0.6455 mL	1.6138 mL
	30 mM	0.0538 mL	0.2690 mL	0.5379 mL	1.3448 mL
	40 mM	0.0403 mL	0.2017 mL	0.4034 mL	1.0086 mL
	50 mM	0.0323 mL	0.1614 mL	0.3228 mL	0.8069 mL
	60 mM	0.0269 mL	0.1345 mL	0.2690 mL	0.6724 mL
	80 mM	0.0202 mL	0.1009 mL	0.2017 mL	0.5043 mL
	100 mM	0.0161 mL	0.0807 mL	0.1614 mL	0.4034 mL

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PLX-4104

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