Cat. No.: HY-190897

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.

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CAS No.: 186036-91-9
Formule: C₂₀H₁₅FN₂O₄
Masse moléculaire:366.34

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Please store the product under the recommended conditions in the Certificate of Analysis.

11F-CPT Chemical Structure

CAS No.: 186036-91-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

Topoisomerase I

Caspase 3

Bax

bad

Bcl-2

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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

Anti-cancerApoptosisCell Cycle RegulationOthers

Anti-cancer

11F-CPT (compound W3) (48 h) is highly cytotoxic in these cancer cell lines, with the lowest IC₅₀ values in UMUC3 and BxPC-3 cells (0.002 μM) and potent activity in A549 cells (0.262 μM)^[1].
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].

Anti-cancer

Apoptosis

11F-CPT (0.01-0.25 μM for BxPC-3; 0.1-2.5 μM for PANC-1; 48 h) induces apoptosis in BxPC-3 and PANC-1 pancreatic cancer cells, increases Bax, Bad, and cleaved caspase-3, and decreases Bcl-2 and increases γ-H2AX protein levels^[1].

Anti-cancer

Cell Cycle Regulation

11F-CPT (0.01-0.25 μM for BxPC-3; 0.1-2.5 μM for PANC-1; 24 h) induces S phase accumulation in BxPC-3 and PANC-1 pancreatic cancer cells and causes G2/M phase arrest at higher concentrations; it also upregulates p53/p21 and CCNA1/CCNB1 and downregulates CCND1/CCNE1^[1].

Others

11F-CPT (0.25-1.5 μM; 30 min) inhibits TOP I-mediated DNA relaxation in a cell-free system^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

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 Proliferation Assay^[1]

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 Cycle Analysis^[1]

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.

Western Blot Analysis^[1]

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.

Apoptosis Analysis^[1]

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.

Western Blot Analysis^[1]

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.

Immunofluorescence^[1]

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

Anti-cancer

11F-CPT (compound W3) (0.3-1.0 mg/kg; i.p.; once every other day; seven doses within 14 days) inhibits the growth of PAN02 subcutaneous tumors in C57BL/6J mice, achieving a tumor inhibition rate of 60.2% at 1.0 mg/kg^[1].

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.

Related Protocols :

Chemical Information

CAS No. 186036-91-9
Masse moléculaire 366.34
Formule C₂₀H₁₅FN₂O₄
SMILES

O=C1C2=C([C@](CC)(O)C(OC2)=O)C=C3C4=NC5=CC(F)=CC=C5C=C4CN31
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Chen GS, et al. Design, Synthesis, and Biological Evaluation of Novel, Fluorinated Camptothecin Derivatives as Potential Topoisomerase I Inhibitors. Journal of medicinal chemistry. 2026 Oct 22;69(20):24030-24052. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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11F-CPT

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