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
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BRD4 2 nM (DC50) |
DCAF11 |
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.
| 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 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID mice with AML MV-4-11 xenografts[1]
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Dosage:2 mg/kg; 6 mg/kg
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Administration:p.o.; daily; 21 days
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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
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CAS No. 2851986-77-9
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Molecular Weight 619.67
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Formula C32H26FN9O2S
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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