Art. -Nr.: HY-183791A

Ferroptosis/apoptosis inducer-5

Ferroptosis/apoptosis inducer-5 is an orally active inducer of Ferroptosis and Apoptosis. Ferroptosis/apoptosis inducer-5 downregulates GPX4, upregulates ACSL4, promotes ROS production, activates the Caspase cascade, induces Mitochondrial dysfunction, and alters the Bcl-2/Bax balance. Ferroptosis/apoptosis inducer-5 significantly inhibits tumor growth in a pancreatic cancer xenograft mouse model. Ferroptosis/apoptosis inducer-5 can be used for the research of pancreatic cancer.

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CAS. Nr.: 2243423-32-5
Formel: C₅₃H₇₂BrO₃P
Molecular Weight:868.01

Speicherung:

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

Data Sheet (281 KB)

Ferroptosis/apoptosis inducer-5 Chemical Structure

CAS. Nr.: 2243423-32-5

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Bax

Bcl-2

GPX4

ACSL4

Alle Glutathione Peroxidase Isoform-spezifische Produkte anzeigen :

GPX1
GPX4

Alle ACSL Family Isoform-spezifische Produkte anzeigen :

ACSL4
ACSL5

Alle Caspase Isoform-spezifische Produkte anzeigen :

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

In Vitro

Ferroptosis/apoptosis inducer-5 (Compound 14) (1.36 μM; 48 h) potently and selectively inhibits the viability of PANC-1 pancreatic cancer cells with an IC₅₀ of 1.36 μM, while showing weaker cytotoxicity against normal 3T3-L1 cells^[1].
Ferroptosis/apoptosis inducer-5 (0.5-2.0 μM; 48 h treatment, followed by 10 days of culture without compound) dose-dependently inhibits the long-term colony-forming ability of PANC-1 pancreatic cancer cells, with near-complete suppression at 2.0 μM^[1].
Ferroptosis/apoptosis inducer-5 (0.125-2.0 μM; 24 h, 48 h) inhibits the proliferation of PANC-1 pancreatic cancer cells in a concentration- and time-dependent manner, with significant effects observed at 0.25-2.0 μM over 48 h^[1].
Ferroptosis/apoptosis inducer-5 (0.125-0.5 μM; 24 h) dose-dependently inhibits the migration and invasive potential of PANC-1 pancreatic cancer cells, with significant effects at 0.5 μM over 24 h^[1].
Ferroptosis/apoptosis inducer-5 (0.5-2.0 μM; 48 h) dose-dependently induces G0/G1 phase arrest in PANC-1 pancreatic cancer cells, inhibiting cell proliferation by blocking completion of the replication cycle^[1].
Ferroptosis/apoptosis inducer-5 (0.5-2.0 μM; 24 h) dose-dependently increases intracellular ROS levels in PANC-1 pancreatic cancer cells, with significant elevation at 0.5 μM over 24 h^[1].
Ferroptosis/apoptosis inducer-5 (0.5-2.0 μM; 48 h) dose-dependently induces apoptosis in PANC-1 pancreatic cancer cells, as evidenced by classical apoptotic morphological changes after 48 h of incubation^[1].
Ferroptosis/apoptosis inducer-5 (0.5-2.0 μM; 24 h) activates the intrinsic mitochondrial apoptotic pathway in PANC-1 pancreatic cancer cells by altering Bcl-2/Bax balance, promoting cytochrome c release, and activating the caspase cascade after 24 h of incubation^[1].
Ferroptosis/apoptosis inducer-5 (0.5-2.0 μM; 24 h) induces ferroptosis in PANC-1 pancreatic cancer cells by downregulating GPX4 and upregulating ACSL4 after 24 h of incubation^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

human pancreatic cancer PANC-1 cells, human choroidal melanoma C918 cells, mouse embryonic fibroblast 3T3-L1 cells
Concentration:

1.36 μM (PANC-1 IC50); 9.25 μM (3T3-L1 IC50)
Incubation Time:

48 h
Result:

Showed potent cytotoxicity against PANC-1 cells with an IC₅₀ of 1.36 μM, far superior to parent betulinic acid (IC₅₀ = 79.29 μM).
Exhibited selective cytotoxicity with an IC₅₀ of 9.25 μM against normal 3T3-L1 cells.
Displayed strong activity against C918 cells.

Cell Proliferation Assay^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.5-2.0 μM
Incubation Time:

48 h treatment, followed by 10 days of culture without compound
Result:

Significantly inhibited PANC-1 colony formation in a concentration-dependent manner.
Almost completely suppressed colony formation at 2.0 μM.

Cell Proliferation Assay^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.125-2.0 μM
Incubation Time:

24 h, 48 h
Result:

Inhibited PANC-1 cell proliferation in a concentration- and time-dependent manner.
Showed no significant effect at 0.125-0.5 μM over 24 h.
Produced significant inhibition at 0.25-2.0 μM over 48 h.

Cell Cycle Analysis^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.5-2.0 μM
Incubation Time:

48 h
Result:

Induced dose-dependent G1 phase arrest in PANC-1 cells.
Increased G1 phase cell percentage.
Decreased S phase cell percentage.
Caused a slight reduction in G2 phase cell percentage.

Apoptosis Analysis^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.5-2.0 μM
Incubation Time:

48 h
Result:

Induced a dose-dependent increase in apoptotic PANC-1 cells.
Caused enhanced blue fluorescence (nuclear condensation/fragmentation) and increased red fluorescence (cell membrane integrity loss).

Western Blot Analysis^[1]

Cell Line:

human pancreatic cancer PANC-1 cells
Concentration:

0.5-2.0 μM
Incubation Time:

24 h
Result:

Dose-dependently upregulated pro-apoptotic Bax and cytosolic cytochrome c.
Downregulated anti-apoptotic Bcl-2.
Increased levels of Cleaved-Caspase-9 and Cleaved-Caspase-3.\nDose-dependently downregulated anti-ferroptotic GPX4.
Upregulated pro-ferroptotic ACSL4.

Parmacokinetics

Species	Dose	Route	T_max	C_max	T_1/2	AUC_0-∞	MRT_0-∞
Rat^[1]	20 mg/kg	p.o.	4.0 h	49.30 μg/mL	5.47 h	337.29 μg·h/mL	7.53 h

In Vivo

Ferroptosis/apoptosis inducer-5 (compound 14) (5-20 mg/kg; i.p.; every 2 days; 28 days) exhibits dose-dependent, significant antitumor activity in a pancreatic cancer xenograft model, achieving a 68.9% tumor weight reduction at the 20 mg/kg dose, while maintaining favorable in vivo safety^[1].

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

Animal Model:

C57BL/6 (female, 6 weeks old, 17-20 g, SPF grade, subcutaneous xenograft model via Panc02 cell injection)^[1]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

i.p.; every 2 days; 28 days
Result:

Reduced tumor weight by 37.1% relative to control.
Reduced tumor weight by 57.0% relative to control.
Reduced tumor weight by 68.9% relative to control, with no significant difference in tumor inhibition rate compared to positive control gemcitabine.
Showed dose-dependent reduction in tumor volume over the 28-day treatment period.
Induced dose-dependent tumor cell apoptosis (increased TUNEL-positive cells), reduced cell proliferation (decreased Ki-67 staining), and downregulated GPX4 expression (indicating ferroptosis induction) in tumor tissues.
Caused no significant pathological abnormalities in heart, liver, spleen, lung, or kidney tissues; serum levels of ALT, AST, BUN, and creatinine were statistically unchanged relative to control.

Related Protocols :

Chemical Information

CAS. Nr. 2243423-32-5
Molecular Weight 868.01
Formel C₅₃H₇₂BrO₃P
SMILES

O=C(OCCCCC[P+](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)[C@@]45CC[C@@]6(C)[C@]7(C)CC[C@@]8([H])C(C)(C)[C@@H](O)CC[C@]8(C)[C@@]7([H])CC[C@]6([H])[C@@]4([H])[C@H](C(C)=C)CC5.[Br-]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhao Y, et al. Design and synthesis of mitochondria-targeted betulinic acid derivatives with antipancreatic cancer activity via ROS-mediated apoptosis and ferroptosis. Bioorg Chem. 2026;177:109934. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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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Ferroptosis/apoptosis inducer-5

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Ferroptosis/apoptosis inducer-5

Alle Glutathione Peroxidase Isoform-spezifische Produkte anzeigen

Alle ACSL Family Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen