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

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 .

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AZ12601011 Chemical Structure

AZ12601011 Chemical Structure

CAS No. : 2748337-86-0

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Based on 3 publication(s) in Google Scholar

AZ12601011 Related Antibodies

Top Publications Citing Use of Products

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • Biological Activity

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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]

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].

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

AZ12601011 Related Antibodies

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].

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

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
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (15.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1912 mL 15.9561 mL 31.9122 mL
5 mM 0.6382 mL 3.1912 mL 6.3824 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1912 mL 15.9561 mL 31.9122 mL 79.7804 mL
5 mM 0.6382 mL 3.1912 mL 6.3824 mL 15.9561 mL
10 mM 0.3191 mL 1.5956 mL 3.1912 mL 7.9780 mL
15 mM 0.2127 mL 1.0637 mL 2.1275 mL 5.3187 mL
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AZ12601011 Related Classifications

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:

AZ126010112748337-86-0AZ 12601011AZ-12601011TGF-β ReceptorTransforming growth factor beta receptorsorallyphosphorylationSMAD2mammarytumorgrowthInhibitorinhibitorinhibit

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