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  3. 8α-Tigloyloxyhirsutinolide 13-O-acetate

8α-Tigloyloxyhirsutinolide 13-O-acetate  (Synonyms: 8αTGH)

Cat. No.: HY-138071
Handling Instructions

8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo.

For research use only. We do not sell to patients.

8α-Tigloyloxyhirsutinolide 13-O-acetate Chemical Structure

8α-Tigloyloxyhirsutinolide 13-O-acetate Chemical Structure

CAS No. : 83182-58-5

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Description

8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo[1][2].

IC50 & Target

STAT3

 

Bcl-2

 

Bcl-xL

 

Mcl-1

 

In Vitro

8α-Tigloyloxyhirsutinolide 13-O-acetate (R001) (0-30 μM, 72 h) dose-dependently suppresses the viable cell numbers of the human cancer lines[1].
8α-Tigloyloxyhirsutinolide 13-O-acetate (0-10 μM, 0-24 h) leads to early pyroptosis and late DNA damage, cell cycle arrest, and apoptosis only in the TNBC cells[1].
8α-Tigloyloxyhirsutinolide 13-O-acetate (0-20 μM, 0-48 h) promotes ROS induction in triple-negative breast cancer cells[1].

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

Cell Proliferation Assay[1]

Cell Line: Multiple human cancer lines, normal human breast epithelial cells and normal human brain microvascular endothelial cells (HBMEC)
Concentration: 0, 1, 2.5, 5, 10, 20, 30 μM
Incubation Time: 72 h
Result: Dose-dependently suppressed the viable cell numbers of the human cancer lines, MDA-MB-468, MDA-MB-231, Panc-1, A549, DU145, HCC1937, and MDA-MB-436 cells with IC50 values of 2.3, 4.4, 4.3, 5.2, 5.8, 6.3, and 7.1 µM, respectively, compared to much weaker effects on the normal human breast epithelial cells, MCF-10A or HBMEC, with IC50 of 23.9 or 14.2 µM, respectively.

Western Blot Analysis[1]

Cell Line: NIH3T3/v-Src fibroblasts, MDA-MB-231, MDA-MB-468, or MCF-10A cells
Concentration: 0, 2, 5, 10, 20 μM
Incubation Time: 30 min, 3 h, 24 h
Result: Suppressed STAT3:STAT3 DNA-binding activity, with IC50 of 5 µM. Showed the inhibition of STAT3 Tyr phosphorylation in time- and dose-dependent manner, while phospho-Ser-STAT3 (pS727-STAT3), pY1068EGFR, and pY-Jak2 were largely unaffected. Attenuated the expression of STAT3 downstream target genes, including c-Myc, Mcl-1, Bcl-2, Bcl-xL, and vascular endothelial growth factor (VEGF) in MDA-MB-468 and MDA-MB-231 cells.

Apoptosis Analysis[1]

Cell Line: Triple-negative breast cancer (TNBC), MDA-MB-231 and MDA-MB-468 cells, or normal human breast epithelial cells, MCF-10A
Concentration: 0, 2.5, 5 or 10 µM
Incubation Time: 6 or 24 h
Result: Showed no significant induction of early apoptosis at 6 h, while the evidence of extensive cell death of 56.2% occurred at later time (24 h), with cleavage of poly (ADP-ribose) polymerase (PARP) and caspase 3 at 24-48 h.
In Vivo

8α-Tigloyloxyhirsutinolide 13-O-acetate (5 mg/kg, Oral gavage, 5 times per week for 75 days) suppresses tumor growth in mice[1].

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

Animal Model: Five-week-old female athymic nude mice (injected subcutaneously in the right flank area with MDA-MB-468 cells in 100 μL PBS)
Dosage: 5 mg/kg
Administration: Oral gavage, every day, 5 times per week for 75 days
Result: Inhibited MDA-MB-468 xenografts growth in mice, with reduced pY705-STAT3, G6PD, TrxR1, and GSH levels.
Molecular Weight

420.45

Formula

C22H28O8

CAS No.
SMILES

O=C(/C(C)=C/C)O[C@@H](C[C@H]1C)C(/C(OC2=O)=C\[C@](O[C@]13O)(CC3)C)=C2COC(C)=O

Structure Classification
Initial Source
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
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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8α-Tigloyloxyhirsutinolide 13-O-acetate
Cat. No.:
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