LGF308
LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: DCAF11 ligand (HY-W288798); Black: linker).
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- CAS No.: 3061406-69-4
- Formule: C35H34ClN7O5S2
- Masse moléculaire:732.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
LGF308 (10 nM-1 μM; 12 h) potently induces BD1 degradation in BD1-HEK293T reporter cells at concentrations as low as 10 nM for 12 h[1].
LGF308 (0.1-5 μM; 3-9 h) induces time- and concentration-dependent degradation of BRD4 in MDA-MB-231 cells, with DC50 values of 0.50 μM (long isoform) and 0.23 μM (short isoform) and maximal degradation of >90% at 5 μM for 9 h[1].
LGF308 (1 μM) induced BRD4 degradation in MDA-MB-231 cells is dependent on the ubiquitin-proteasome pathway, not the lysosomal pathway[1].
LGF308 (0.1-10 μM; 12 h) induces BRD4/BD1 degradation in BD1-HEK293T and CRISPRi HEK293T cells that is DCAF11-dependent[1].
LGF308 (1 μM; 6 h) promotes formation of a ternary complex between BD1 and DCAF11 in HEK293T cells[1].
LGF308 (gradient concentrations; 48 h) selectively inhibits proliferation of breast cancer cell lines, with the highest potency in MDA-MB-468 cells (IC50=0.70 μM) and lower potency in normal HEK293T cells (IC50=16.01 μM) after 48 h treatment[1].
LGF308 (1 μM) induces apoptosis in MDA-MB-231 cells, as shown by upregulated c-PARP-1 and c-Caspase-7 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.1 μM, 0.5 μM, 1 μM, 2 μM, 5 μM (9 h treatment); 1 μM (3 h, 6 h, 9 h treatments)
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Incubation Time:3 h, 6 h, 9 h (1 μM treatment); 9 h (0.1-5 μM treatments)
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Result:Reduced BRD4 levels to ~60% of control after 3 h of 1 μM treatment.
Dropped BRD4 levels to ~40% of control by 6 h of 1 μM treatment.
Degraded over 90% of both long and short BRD4 isoforms at 5 μM, with a DC50 of 0.50 μM for the long isoform and 0.23 μM for the short isoform.
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Cell Line:MCF-7, T-47D, MDA-MB-231, MDA-MB-157, MDA-MB-468, HCC1937, BT-549 (breast cancer cell lines), HEK293T (normal cell line)
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Concentration:Gradient concentrations
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Incubation Time:48 h
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Result:Inhibited proliferation of breast cancer cell lines with IC50 values of 2.86 μM (MCF-7), 2.22 μM (T-47D), 1.31 μM (MDA-MB-231), 3.10 μM (MDA-MB-157), 0.70 μM (MDA-MB-468), 1.45 μM (HCC1937), 1.60 μM (BT-549).
Resulted in an IC50 of 16.01 μM for normal HEK293T cells, significantly higher than cancer cell lines.
| Species | Dose | Route | T1/2 | Vdss | MRT0-inf | CL | Cmax | AUC0-t | AUC0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 3 mg/kg | i.v. | 3.84 h | 0.08 L/kg | 1.72 h | 0.73 mL/min/kg | 30,833.3 ng/mL | 114,985 | 115,124 |
Chemical Information
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CAS No. 3061406-69-4
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Masse moléculaire 732.27
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Formule C35H34ClN7O5S2
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SMILES
O=C(N1CCCCCCNC(C[C@@H]2N=C(C3=C(N4C2=NN=C4C)SC(C)=C3C)C5=CC=C(C=C5)Cl)=O)/C(SC1=O)=C/C6=CC([N+]([O-])=O)=CC=C6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LGF308 Related Classifications
HY-181756 Related Classifications
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