1. TGF-beta/Smad
  2. TGF-β Receptor
  3. AZ12601011

AZ12601011 

Cat. No.: HY-122856
Handling Instructions

AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .

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

AZ12601011 Chemical Structure

AZ12601011 Chemical Structure

Size Stock
100 mg Get quote
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth [1].

IC50 & Target[1]

TGFBR1

18 nM (IC50)

TGFBR1

2.9 nM (Kd)

ALK4

 

ALK7

 

In Vitro

AZ12601011 (0.01-10 μM; for 20 minutes) completely inhibits Phosphorylation of SMAD2 [1].
AZ12601011 (0.01 µM-10 µM) inhibits the activity of ALK4, ALK7 and TGFBR1 [1].
AZ12601011 inhibits 4T1 cells growth in vitro (IC50=0.4µM) [1].

Western Blot Analysis[1]

Cell Line: NIH3T3, HaCaT, C2C12, T47D cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 20 minutes
Result: Completely inhibited Phosphorylation of SMAD2.
In Vivo

AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo[1].

Animal Model: Female BALB/c mice at greater than 18g with tumour[1]
Dosage: 50mg/kg
Administration: Oral gavage; twice daily; for 25 days
Result: Inhibited tumour growth and metastasis in vivo.
Molecular Weight

313.36

Formula

C₁₉H₁₅N₅

SMILES

C1(C2=NC=CC=C2)=NC(N3C=CC4=C3C=CN=C4)=C(CCC5)C5=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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.
  • 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

Keywords:

AZ12601011AZ 12601011AZ-12601011TGF-β ReceptorTransforming growth factor beta receptorsorallyphosphorylationSMAD2mammarytumorgrowthInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
AZ12601011
Cat. No.:
HY-122856
Quantity:
MCE Japan Authorized Agent: