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

AZ12601011 

Cat. No.: HY-122856 Purity: 99.25%
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 Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 385 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2150 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE AZ12601011

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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].

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

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].

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (15.96 mM; Need ultrasonic)

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
10 mM 0.3191 mL 1.5956 mL 3.1912 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
AZ12601011
Cat. No.:
HY-122856
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