11F-CPT
11F-CPT is a Topoisomerase I inhibitor that stabilizes the TOP I-DNA cleavage complex. 11F-CPT inhibits TOP I-mediated DNA relaxation, induces DNA damage, and activates ATR-CHK1 signaling. 11F-CPT selectively inhibits proliferation and colony formation in pancreatic cancer cells, upregulates γ‑H2AX, and induces cell cycle arrest and apoptosis. 11F-CPT inhibits tumor growth in the PAN02 pancreatic cancer xenograft model and enhances the thermal stability of TOP I in cells. 11F-CPT can be used for research on pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 186036-91-9
- Formula: C20H15FN2O4
- Molecular Weight:366.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Topoisomerase I |
Caspase 3 |
Bax |
bad |
Bcl-2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
0.110 μM
|
Antiproliferative activity against human HepG2 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human HepG2 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| A549 | IC50 |
0.262 μM
|
Antiproliferative activity against human A549 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human A549 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| MCF7 | IC50 |
0.205 μM
|
Antiproliferative activity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| SW480 | IC50 |
0.101 μM
|
Antiproliferative activity against human SW480 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human SW480 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| T-24 | IC50 |
0.006 μM
|
Antiproliferative activity against human T24 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human T24 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| UMUC3 | IC50 |
0.002 μM
|
Antiproliferative activity against human UMUC3 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human UMUC3 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| PANC-1 | IC50 |
0.164 μM
|
Antiproliferative activity against human PANC-1 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human PANC-1 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| BXPC-3 | IC50 |
0.002 μM
|
Antiproliferative activity against human BxPC-3 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human BxPC-3 cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
| L02 | IC50 |
0.0193 μM
|
Cytotoxicity against normal human L02 liver cells assessed as viability reduction incubated 48 hrs by MTT assay.
Cytotoxicity against normal human L02 liver cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42911683 |
In Vitro
11F-CPT (0.01-0.25 μM for BxPC-3; 0.1-2.5 μM for PANC-1; 24 h-14 days) reduces EdU incorporation and decreases colony formation in BxPC-3 and PANC-1 pancreatic cancer cells[1].
11F-CPT (0.01 μM for BxPC-3; 0.1 μM for PANC-1; 48 h) increases the proportion of γ-H2AX-positive BxPC-3 and PANC-1 pancreatic cells[1].
11F-CPT (0.5 μM for BxPC-3; 2.5 μM for PANC-1) inhibits the catalytic activity of TOP I in BxPC-3 and PANC-1 pancreatic cancer cells[1].
11F-CPT enhances the thermal stability of TOP I in BxPC-3 pancreatic cancer cells and increases the DNA-bound TOP I[1].
11F-CPT (0.1 μM) increases γ-H2AX and activates p-ATR/p-CHK1 signaling in BxPC-3 pancreatic cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:BxPC-3 and PANC-1 human pancreatic cancer cells
-
Concentration:0.01, 0.05, and 0.25 μM (BxPC-3)
0.1, 0.5, and 2.5 μM (PANC-1) -
Incubation Time:24 h
-
Result:Reduced EdU incorporation in BxPC-3 and PANC-1 pancreatic cancer cells.
-
Cell Line:BxPC-3 and PANC-1 human pancreatic cancer cells
-
Concentration:0.01, 0.05, and 0.25 μM (BxPC-3)
0.1, 0.5, and 2.5 μM (PANC-1) -
Incubation Time:14 days
-
Result:Markedly reduced colony numbers in BxPC-3 cells.
Suppressed colony formation in PANC-1 cells.
-
Cell Line:BxPC-3 and PANC-1 human pancreatic cancer cells
-
Concentration:0.01, 0.05, and 0.25 μM (BxPC-3)
0.1, 0.5, and 2.5 μM (PANC-1) -
Incubation Time:24 h
-
Result:Induced S-phase accumulation and G2/M arrest at higher concentrations in BxPC-3 and PANC-1 pancreatic cancer cells.
-
Cell Line:BxPC-3 and PANC-1 human pancreatic cancer cells
-
Concentration:0.01, 0.05, and 0.25 μM (BxPC-3)
0.1, 0.5, and 2.5 μM (PANC-1) -
Incubation Time:24 h
-
Result:Upregulated p53/p21 and CCNA1/CCNB1, while downregulating CCND1/CCNE1.
-
Cell Line:BxPC-3 and PANC-1 human pancreatic cancer cells
-
Concentration:0.01, 0.05, and 0.25 μM (BxPC-3)
0.1, 0.5, and 2.5 μM (PANC-1) -
Incubation Time:48 h
-
Result:Induced apoptosis in BxPC-3 and PANC-1 pancreatic cancer cells, reaching total apoptosis rates of 56.2% and 41.6%, respectively.
-
Cell Line:BxPC-3 and PANC-1 human pancreatic cancer cells
-
Concentration:0.01, 0.05, and 0.25 μM (BxPC-3)
0.1, 0.5, and 2.5 μM (PANC-1) -
Incubation Time:48 h
-
Result:Increased the levels of Bax, Bad, and cleaved caspase-3, and decreases the level of Bcl-2.
Increased γ-H2AX protein levels in BxPC-3 and PANC-1 pancreatic cancer cells.
-
Cell Line:BxPC-3 and PANC-1 human pancreatic cancer cells
-
Concentration:0.01 μM (BxPC-3)
0.1 μM (PANC-1) -
Incubation Time:48 h
-
Result:Increased the proportion of γ-H2AX-positive BxPC-3 cells at 0.01 μM and markedly increased γ-H2AX-positive PANC-1 cells at 0.1 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J (female, 2 × 106 PAN02 cells in 150 μL)[1]
-
Dosage:0.3, 1.0 mg/kg
-
Administration:i.p.; every other day; seven doses over 14 days
-
Result:Inhibited tumor growth substantially at all tested doses, as assessed by tumor volume and tumor weight.
Reached tumor inhibition rates of 42.4% at 0.3 mg/kg and 60.2% at 1.0 mg/kg at the Day 14 endpoint.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Soft Agar Colony Formation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Genotoxicity/Mutagenicity Study
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 186036-91-9
-
Molecular Weight 366.34
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Formula C20H15FN2O4
-
SMILES
O=C1C2=C([C@](CC)(O)C(OC2)=O)C=C3C4=NC5=CC(F)=CC=C5C=C4CN31
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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)