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PLX-4104

Catalog No.GC80929 Copy One-Click Copy Product Info

PLX-4104 is an orally active BRD4 molecular glue degrader with a DC50 of 2 nM.

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PLX-4104 Chemical Structure

Cas No.: 2851986-77-9

Taille Prix Stock Qté
5mg
396,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.



Description of 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 [1].

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].

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].

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

Chemical Properties of PLX-4104

Cas No. 2851986-77-9 SDF
Formula C32H26FN9O2S M.Wt 619.67
Solubility DMSO: 100 mg/mL (161.38 mM; Need ultrasonic) Storage Store at -20°C
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of PLX-4104

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1 mg 5 mg 10 mg
1 mM 1.6138 mL 8.0688 mL 16.1376 mL
5 mM 322.8 μL 1.6138 mL 3.2275 mL
10 mM 161.4 μL 806.9 μL 1.6138 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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