2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. STAT c-Myc CDK Oxidative Phosphorylation
  4. 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.

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

STAT3-IN-32

STAT3-IN-32 Chemical Structure

CAS No. : 2591440-71-8

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

STAT3-IN-32 Related Antibodies

Top Publications Citing Use of Products

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

STAT3

 

Cellular Effect
Cell Line Type Value Description References
BXPC-3 IC50
0.4 nM
Compound: 4c
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
[PMID: 36282975]
BXPC-3 IC50
4.2 nM
Compound: 4c
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
[PMID: 36282975]
Capan-2 IC50
1.9 nM
Compound: 4c
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
[PMID: 36282975]
CFPAC-1 IC50
6 nM
Compound: 4c
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
[PMID: 36282975]
MIA PaCa-2 IC50
2.1 nM
Compound: 4c
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
[PMID: 36282975]
PC-3 IC50
>1000 nM
Compound: 4c
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
[PMID: 36282975]
PC-3 IC50
>1 μM
Compound: 4c
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
[PMID: 36282975]
In Vitro

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.

STAT3-IN-32 Related Antibodies

Western Blot Analysis[1]

Cell Line: BxPC-3, Capan-2 pancreatic cancer cells; PC-3 STAT3-negative cells
Concentration: 0; 1; 3; 10; 30; 100; 300; 1000
Incubation Time: 0; 4; 8; 12; 16; 20; 24 h
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.
Parmacokinetics
Species Dose Route Cmax AUC0-24 AUC0-∞ Vd CL MRTlast T1/2 F
Mice[1] 1 mg/kg i.v. 2568.1 ng/mL 9506.6 ng·h/mL 11643.9 ng·h/mL 1267.6 mL/kg 85.9 mL/h/kg 8.1 h 10.2 h /
Mice[1] 10 mg/kg p.o. 1805.5 ng/mL 27642.1 ng·h/mL 34915.2 ng·h/mL / / 9.8 h 9.4 h 29.1 %
In Vivo

STAT3-IN-32 (compound 4c) (10-30 mg/kg; p.o.; daily; 8 weeks) exhibits potent dose-dependent antitumor efficacy in a mouse BxPC-3 pancreatic cancer xenograft model[1].

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

Animal Model: Male BALB/c-nude mice (6-8 weeks old) injected with BxPC-3 cells[1]
Dosage: 10; 30 mg/kg
Administration: p.o.; daily; 8 weeks
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.
Molecular Weight

699.68

Formula

C36H32F3N7O5
CAS No.
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
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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

STAT3-IN-32 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

STAT3-IN-322591440-71-8STATc-MycCDKOxidative PhosphorylationMycCyclin dependent kinasepancreatic cancerSer727MIA PaCa-2HEK293T cellsSTAT3 SH2 domainCapan-2BxPC-3Tyr705PC-3CFPAC-1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
STAT3-IN-32
Cat. No.:
HY-164445
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.