2. TGF-beta/Smad
  3. TGF-β Receptor
  4. AZ12799734

AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor.

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

AZ12799734 Chemical Structure

AZ12799734 Chemical Structure

CAS No. : 1117684-36-2

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Customer Review

Based on 1 publication(s) in Google Scholar

AZ12799734 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

  • Purity & Documentation

  • References

  • Customer Review

Description

AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor[1].

IC50 & Target

TGFBR1

47 nM (IC50)

ALK6

0.017 μM (Kd)

ALK5

0.74 μM (Kd)

ALK4

1 μM (Kd)

ACVR1

6.2 μM (Kd)

ALK1

7.1 μM (Kd)

BMPR1A

40 μM (Kd)

BMP

 

Cellular Effect
Cell Line Type Value Description References
MDA-MB-468 IC50
22 nM
Compound: 19
Inhibition of ALK5 in human MDA-MB-468 cells assessed as inhibition of nuclear translocation of GFP-2/Smad2 fusion reporter gene after 90 mins by Hoechst 3342 staining-based cellomics arrayscan imaging analysis
Inhibition of ALK5 in human MDA-MB-468 cells assessed as inhibition of nuclear translocation of GFP-2/Smad2 fusion reporter gene after 90 mins by Hoechst 3342 staining-based cellomics arrayscan imaging analysis
[PMID: 19736928]
Sf21 IC50
72 nM
Compound: 19
Inhibition of 6His-tagged human ALK5 expressed in baculovirus-infected SF21 cells after 30 mins by fluorescence polarization assay
Inhibition of 6His-tagged human ALK5 expressed in baculovirus-infected SF21 cells after 30 mins by fluorescence polarization assay
[PMID: 19736928]
In Vitro

AZ12799734 inhibits ligand activated SMAD3/4 transcription[1].
AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[1].
AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[1].

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

AZ12799734 Related Antibodies

Western Blot Analysis[1]

Cell Line: HaCaT cells and NIH3T3 cells
Concentration: 10 nM
Incubation Time: 10 days (HaCaT) or 24 h (NIH3T3)
Result: Blocked TGFβ-mediated induction of SMAD2 phosphorylation. Inhibited phosphorylation of both SMAD1 and SMAD2.

Cell Migration Assay [1]

Cell Line: HaCaT epithelial cells
Concentration: 500 nM
Incubation Time: 36 h
Result: A dose-dependent decrease in TGFβ-induced migration was observed.
In Vivo

AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat[2].
AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC50 of 0.01885 μM[1].

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

Animal Model: Ten-week-old female HsdHan:WIST rats[2]
Dosage: 200 and 400 mg/kg/day
Administration: Oral, 3-7 days
Result: Hemorrhage into the heart valves was evident at low magnification and the normal architecture of the leaflet was replaced by hemorrhage.
Increased valvular interstitial cells in size and number and shows increased cytoplasm, an enlarged round to spindeloid nucleus, and frequently undergoing mitosis.
Animal Model: Female BALB/c mice[1]
Dosage: 50 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: Showed total and free pharmacokinetic (PK) levels with time over in vitro IC50 of 0.01885 μM.
Molecular Weight

370.43

Formula

C18H18N4O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(NC2=NC=CC(OC3=CC=C(C)N=C3C)=C2)C=C1)(N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (337.45 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 2.6996 mL 13.4978 mL 26.9957 mL
5 mM 0.5399 mL 2.6996 mL 5.3991 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Please enter the basic information of animal experiments:

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Calculation results:
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6996 mL 13.4978 mL 26.9957 mL 67.4891 mL
5 mM 0.5399 mL 2.6996 mL 5.3991 mL 13.4978 mL
10 mM 0.2700 mL 1.3498 mL 2.6996 mL 6.7489 mL
15 mM 0.1800 mL 0.8999 mL 1.7997 mL 4.4993 mL
20 mM 0.1350 mL 0.6749 mL 1.3498 mL 3.3745 mL
25 mM 0.1080 mL 0.5399 mL 1.0798 mL 2.6996 mL
30 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2496 mL
40 mM 0.0675 mL 0.3374 mL 0.6749 mL 1.6872 mL
50 mM 0.0540 mL 0.2700 mL 0.5399 mL 1.3498 mL
60 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
80 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8436 mL
100 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6749 mL
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AZ12799734 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:

AZ127997341117684-36-2AZ 12799734AZ-12799734TGF-β ReceptorTransforming growth factor beta receptorsHaCaTSMAD1SMAD2SMAD3/4TGFBR1BMPheart valve lesionsInhibitorinhibitorinhibit

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