PROTAC FGFR1 degrader-1
PROTAC FGFR1 degrader-1 is a PROTAC degrader targeting fibroblast growth factor receptor 1 (FGFR1), with a DC50 of 39.78 nM and an IC50 of 26.81 nM in KG1a cells. PROTAC FGFR1 degrader-1 selectively degrades FGFR1 via the ubiquitin-proteasome system, showing concentration- and time-dependent degradation in cancer cells. PROTAC FGFR1 degrader-1 can be used in studies related to leukemia and breast cancer.
(Pink: FGFR Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker (HY-W007587)).
For research use only. We do not sell to patients.
- Formula: C46H54N8O8
- Molecular Weight:846.97
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- References
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Biological Activity
Description
IC50 & Target
[1]|
FGFR1 39.78 nM (DC50) |
FGFR1 26.81 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KG-1a | DC50 |
39.78 nM
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Half-maximal FGFR1 degradation in human KG1a leukemia cells assessed by western blot after 24 h incubation.
Half-maximal FGFR1 degradation in human KG1a leukemia cells assessed by western blot after 24 h incubation.
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39756204 |
| KG-1a | IC50 |
26.81 nM
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Antiproliferative activity against human KG1a leukemia cells assessed by CCK-8 assay.
Antiproliferative activity against human KG1a leukemia cells assessed by CCK-8 assay.
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39756204 |
| MCF7 | IC50 |
> 20 μM
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Antiproliferative activity against human MCF-7 breast cancer cells assessed by CCK-8 assay, with no observed activity at concentrations up to 20 μM.
Antiproliferative activity against human MCF-7 breast cancer cells assessed by CCK-8 assay, with no observed activity at concentrations up to 20 μM.
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39756204 |
In Vitro
PROTAC FGFR1 degrader-1 (compound S2h) (1 μM; 72 h) degrades 71.7% of FGFR1 protein in MCF-7 cells[1].
PROTAC FGFR1 degrader-1 (0.1-1 μM; 24 h) induces significant concentration-dependent degradation of FGFR1 protein in KG1a cells[1].
PROTAC FGFR1 degrader-1 (0.1-10 μM; 72 h) selectively degrades FGFR1 (but not FGFR2, FGFR3 or FGFR4) in MCF-7 cells in a dose-dependent manner in vitro[1].
PROTAC FGFR1 degrader-1 (7.8-500 nM; 24 h) induces concentration-dependent FGFR1 degradation in KG1a cells, with a DC50 of 39.78 nM and a Dmax of 78%[1].
PROTAC FGFR1 degrader-1 (250 nM; 6-48 h) induces time-dependent degradation of FGFR1 in KG1a cells, with a significant reduction observed at 9 h and the maximum degradation achieved at 24 h[1].
PROTAC FGFR1 degrader-1 potently inhibits the proliferation of KG1a cells with an IC50 of 26.81 nM, but shows no activity against MCF-7 cells[1].
PROTAC FGFR1 degrader-1 (250-1000 nM; 24 h) induces dose-dependent G0/G1 cell cycle arrest in KG1a cells[1].
PROTAC FGFR1 degrader-1 (62.5-500 nM; 72 h) induces dose-dependent apoptosis in KG1a cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:1 μM
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Incubation Time:72 h
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Result:Induced degradation of 71.7% of FGFR1 protein in MCF-7 cells.
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Cell Line:KG1a human leukemia cells
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Concentration:0.1, 0.5, 1 μM
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Incubation Time:24 h
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Result:Induced significant concentration-dependent degradation of FGFR1 protein in KG1a cells.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:0.1,1, 10 μM
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Incubation Time:72 h
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Result:Selectively degraded FGFR1 in a dose-dependent manner.
No significant degradation of FGFR2, FGFR3, or FGFR4 was observed.
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Cell Line:KG1a human leukemia cells
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Concentration:7.8, 15.6, 31.2, 62.5, 125, 250, 500 nM
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Incubation Time:24 h
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Result:Induced concentration-dependent FGFR1 degradation with no observed hook effect below 125 nM.
Achieved a half-maximal degradation concentration (DC50) of 39.78 nM and a maximum degradation level (Dmax) of 78%.
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Cell Line:KG1a human leukemia cells
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Concentration:250 nM
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Incubation Time:6, 9, 12, 24, 48 h
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Result:Induced time-dependent FGFR1 degradation, with significant reduction observed at 9 h and maximum degradation achieved at 24 h.
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Cell Line:KG1a human leukemia cells
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Concentration:250 nM (12 h incubation); 1 μM (72 h incubation)
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Incubation Time:12, 72 h
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Result:Pretreatment with MG132 completely blocked S2h-induced FGFR1 degradation.
Pretreatment with AZD4547 or pomalidomide notably inhibited degradation.
The negative control S2h-NEG showed significantly decreased FGFR1 degradation activity compared to S2h.
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Cell Line:KG1a human leukemia cells
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Concentration:250, 500, 1000 nM
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Incubation Time:24 h
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Result:Induced weak G0/G1 phase cell cycle arrest at 250 nM, with significantly enhanced arrest at higher concentrations.
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Cell Line:KG1a human leukemia cells
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Concentration:62.5, 125, 500 nM
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Incubation Time:72 h
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Result:Induced significant dose-dependent apoptosis of KG1a cells.
26.31% of cells underwent apoptosis at 500 nM, which was higher than the 15.8% apoptosis induced by 500 nM AZD4547.
Chemical Information
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Molecular Weight 846.97
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Formula C46H54N8O8
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SMILES
O=C(NC1=NNC(CCC2=CC(OC)=CC(OC)=C2)=C1)C3=CC=C(N4CCN(CCCCCCCCC(NC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)CC4)C=C3
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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)
PROTAC FGFR1 degrader-1 Related Classifications
HY-170869 Related Classifications
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