STAT3-IN-32
STAT3-IN-32 is an orally active, selective STAT3 SH2 domain inhibitor with a Kd of 21.3 nM, showing selectivity over STAT1/5. STAT3-IN-32 binds to the STAT3 SH2 domain, blocks Tyr705 and Ser727 phosphorylation, abrogates nuclear transcription and mitochondrial oxidative phosphorylation functions. STAT3-IN-32 inhibits tumor growth in mouse pancreatic cancer xenograft models. STAT3-IN-32 can be used for the research of pancreatic cancer.
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- CAS. Nr.: 2591440-71-8
- Formel: C36H32F3N7O5
- Molecular Weight:699.68
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
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STAT3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | IC50 |
0.4 nM
Compound: 4c
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Anti-proliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
Anti-proliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
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[PMID: 36282975] |
| BXPC-3 | IC50 |
4.2 nM
Compound: 4c
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Inhibition of ATP production in human BXPC-3 cells incubated for 20 to 24 hrs by ATP assay kit method
Inhibition of ATP production in human BXPC-3 cells incubated for 20 to 24 hrs by ATP assay kit method
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[PMID: 36282975] |
| Capan-2 | IC50 |
1.9 nM
Compound: 4c
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Anti-proliferative activity against human Capan-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
Anti-proliferative activity against human Capan-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
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[PMID: 36282975] |
| CFPAC-1 | IC50 |
6 nM
Compound: 4c
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Anti-proliferative activity against human CFPAC-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
Anti-proliferative activity against human CFPAC-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
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[PMID: 36282975] |
| MIA PaCa-2 | IC50 |
2.1 nM
Compound: 4c
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Anti-proliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
Anti-proliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
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[PMID: 36282975] |
| PC-3 | IC50 |
>1000 nM
Compound: 4c
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Anti-proliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
Anti-proliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
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[PMID: 36282975] |
STAT3-IN-32 (compound 4c) potently inhibits STAT3 luciferase activity in HEK293T cells with an IC50 of 5.3 nM[1].
STAT3-IN-32 inhibits ATP production in BxPC-3 pancreatic cancer cells with an IC50 of 4.2 nM[1].
STAT3-IN-32 potently inhibits proliferation of STAT3-dependent BxPC-3, Capan-2, CFPAC-1, and MIA PaCa-2 pancreatic cancer cells with single-digit to low nanomolar IC50 values, but does not affect STAT3-negative PC-3 cell proliferation[1].
STAT3-IN-32 does not inhibit human CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4-M isoforms at concentrations up to 50 μM[1].
STAT3-IN-32 (0-1000 nM; 0-24 h) concentration- and time-dependently inhibits STAT3 Tyr705 and Ser727 phosphorylation and downstream c-Myc and Cyclin D1 expression in BxPC-3 and Capan-2 pancreatic cancer cells without altering total STAT3 levels, and has no effect on c-Myc or Cyclin D1 in STAT3-negative PC-3 cells[1].
STAT3-IN-32 does not inhibit STAT3 upstream kinases JAK1, JAK2, EGFR, SRC, ERK1, JNK1, or P38δ at concentrations up to 10 μM[1].
STAT3-IN-32 (0-30 nM) concentration-dependently blocks IL-6-induced STAT3 Tyr705 phosphorylation and subsequent nuclear translocation in BxPC-3 and Capan-2 pancreatic cancer cells[1].
STAT3-IN-32 (0-30 nM) concentration-dependently inhibits mitochondrial respiration, including basal respiration, maximal respiration, and ATP production-linked oxygen consumption, in BxPC-3 and CFPAC-1 pancreatic cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC-3, Capan-2 pancreatic cancer cells; PC-3 STAT3-negative cells
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Concentration:0; 1; 3; 10; 30; 100; 300; 1000
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Incubation Time:0; 4; 8; 12; 16; 20; 24 h
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Result:Inhibited STAT3 phosphorylation at Tyr705 and Ser727 in a concentration- and time-dependent manner, with complete inhibition of both phosphorylation sites at 10 nM.
Did not affect total STAT3 protein levels.
Suppressed expression of STAT3 downstream target genes c-Myc and Cyclin D1 in a concentration- and time-dependent manner.
In STAT3-negative PC-3 cells, up to 1000 nM STAT3-IN-32 had no effect on c-Myc or Cyclin D1 expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c-nude mice (6-8 weeks old) injected with BxPC-3 cells[1]
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Dosage:10; 30 mg/kg
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Administration:p.o.; daily; 8 weeks
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Result:Achieved a tumor growth inhibition (TGI) rate of 69.2% at 10 mg/kg.
Achieved a TGI rate of 74.6% at 30 mg/kg.
Strongly inhibited STAT3 phosphorylation at Tyr705 and Ser727 in tumor tissues with no significant effect on total STAT3 levels.
Effectively suppressed Ki67 expression in tumor tissues.
Chemical Information
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CAS. Nr. 2591440-71-8
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Molecular Weight 699.68
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Formel C36H32F3N7O5
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SMILES
O=C(C(N1C)=CC2=C1C=C(OC3=NC=C(C4=NC(C5=CC=C(OC)C=C5)=NO4)N=C3)C=C2)N6CCN(CC7=CC=C(OCC(F)(F)F)C=C7)CC6
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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