GXF-111
GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer.
(Pink: BRD3 and BRD4-L Target protein ligand; Blue: Cereblon ligand (HY-138793); Black: linker).
For research use only. We do not sell to patients.
- Formula: C42H42ClN7O3
- Molecular Weight:728.28
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
Ki: 11.97 nM (BRD3 BD1); 2.35 nM (BRD3 BD2) [1].
IC50: 6.31 nM (MV4-11 cell); 95.2 nM (MM.1 S cell) [1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
14.26 μM
Compound: 24; GXF111
|
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
|
[PMID: 37084596] |
| HeLa | IC50 |
6.96 μM
Compound: 24; GXF111
|
Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
|
[PMID: 37084596] |
| HepG2 | IC50 |
17.25 μM
Compound: 24; GXF111
|
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
|
[PMID: 37084596] |
| HGC-27 | IC50 |
2.35 μM
Compound: 24; GXF111
|
Antiproliferative activity against human HGC-27 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
Antiproliferative activity against human HGC-27 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
|
[PMID: 37084596] |
| MCF7 | IC50 |
0.23 μM
Compound: 24; GXF111
|
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay
|
[PMID: 37084596] |
| MM1.S | IC50 |
95.2 nM
Compound: 24; GXF111
|
Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 4 days by CellTitre-Glo assay
Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 4 days by CellTitre-Glo assay
|
[PMID: 37084596] |
| MV4-11 | IC50 |
6.31 nM
Compound: 24; GXF111
|
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 3 days by CellTitre-Glo assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 3 days by CellTitre-Glo assay
|
[PMID: 37084596] |
GXF-111 (Compound 24) has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively[1].
GXF-111 has cellular activities in MV4-11 and MM.1 S cell lines with IC50 values of 6.31 nM and 95.2 nM, respectively[1].
GXF-111 (2, 10 nM; 24 h) has potent cell growth inhibition activities for degradation of BET family proteins in MM.1 S cells[1].
GXF-111 (4 days) has anti-proliferative activity in 7 human cancer cell lines with IC50 values range from 6.31 nM to 17.25 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MM.1 S cells；MM.1 S, HGC-27, and MCF-7 cells；Multiple cancer cell lines
-
Concentration:2, 10 nM; 0.1, 0.3, 1, 3 nM; 30 nM; 3, 10, 30, 100, 300 nM
-
Incubation Time:24 h; 8 h; 1, 3, 6, 8, 24 h; 24 h
-
Result:Efficiently depleted BRD3 and BRD4-L in MM.1 S cells at 2 nM.
Dose-dependently depleted BRD3 and BRD4-L and partially depleted BRD2 at 10 nM.
Had good degradation kinetics of BET proteins in three selected cancer cell lines, i.e. MM.1S, MCF-7, and HGC-27 cells.
Only BRD3 and BRD4-L, were depleted dose-dependently in five cancer cell lines, i.e. HGC27, MCF-7, A549, Hela, and HepG2 cells.
-
Cell Line:MM.1 S cell
-
Concentration:1, 3, 10, 30, 100, 300 nM
-
Incubation Time:24 h
-
Result:Dose-dependently induced cell cycle arrest at G1 phase.
Chemical Information
-
Molecular Weight 728.28
-
Formula C42H42ClN7O3
-
SMILES
O=C1N(C2C(NC(CC2)=O)=O)CC3=C1C=CC=C3CCCCNCC4=CC=C(C5=CC=C6C(C(NC7=CC=C(Cl)C=C7)CCC8=NN=C(C)N86)=C5)C=C4
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)
Powered by Bioz