AZ12799734
Based on 1 Customer Validation
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.
- Purity: 98.67%
- CAS No.: 1117684-36-2
- Formula: C18H18N4O3S
- Molecular Weight:370.43
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Kinase Inhibitor Library
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Biological Activity
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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 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-468 | IC50 |
22 nM
Compound: 19
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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
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[PMID: 19736928] |
| Sf21 | IC50 |
72 nM
Compound: 19
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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
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[PMID: 19736928] |
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.
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Cell Line:HaCaT cells and NIH3T3 cells
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Concentration:10 nM
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Incubation Time:10 days (HaCaT) or 24 h (NIH3T3)
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Result:Blocked TGFβ-mediated induction of SMAD2 phosphorylation. Inhibited phosphorylation of both SMAD1 and SMAD2.
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Cell Line:HaCaT epithelial cells
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Concentration:500 nM
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Incubation Time:36 h
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Result:A dose-dependent decrease in TGFβ-induced migration was observed.
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.
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Animal Model:Ten-week-old female HsdHan:WIST rats[2]
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Dosage:200 and 400 mg/kg/day
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Administration:Oral, 3-7 days
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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.
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Animal Model:Female BALB/c mice[1]
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Dosage:50 mg/kg
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Administration:Oral administration (Pharmacokinetic Analysis)
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Result:Showed total and free pharmacokinetic (PK) levels with time over in vitro IC50 of 0.01885 μM.
Chemical Information
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CAS No. 1117684-36-2
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Appearance Solid
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Molecular Weight 370.43
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Formula C18H18N4O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(NC2=NC=CC(OC3=CC=C(C)N=C3C)=C2)C=C1)(N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor β Superfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234. [Content Brief]
[2]. Anderton MJ, et al. Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol Pathol. 2011 Oct;39(6):916-24. [Content Brief]
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 |
AZ12799734 Related Classifications
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