2. PROTAC Epigenetics
  3. Molecular Glues Epigenetic Reader Domain
  4. 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.

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PLX-4104

PLX-4104 Chemical Structure

CAS No. : 2851986-77-9

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PLX-4104 Related Antibodies

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Description

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].

IC50 & Target[1]

BRD4

2 nM (DC50)

DCAF11

 

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.

PLX-4104 Related Antibodies
Parmacokinetics
Species Dose Route CL T1/2 Vss AUC0-inf Cmax Tmax 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.
Molecular Weight

619.67

Formula

C32H26FN9O2S
CAS No.
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
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Storage

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References
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PLX-4104 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PLX-41042851986-77-9PLX4104PLX 4104Molecular GluesEpigenetic Reader Domainproteasomal breakdowncancer cell proliferationCaco-2 cellshuman liver microsomesubiquitinationacute myeloid leukemiaBRD4mouse liver microsomesMV-4-11 cellsDCAF11Inhibitorinhibitorinhibit

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