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AZ 12799734
🥰Excellent
Catalog No. T35896Cas No. 1117684-36-2
Alias AZ12799734
AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.
AZ 12799734
🥰Excellent
Purity: 98.23%
Catalog No. T35896Alias AZ12799734Cas No. 1117684-36-2
AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $113 | In Stock | |
| 10 mg | $185 | In Stock | |
| 25 mg | $397 | In Stock | |
| 50 mg | $662 | In Stock | |
| 100 mg | $926 | In Stock | |
| 500 mg | $1,850 | In Stock |
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A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.
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CitedCrizotinib Cited
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Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.
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CitedDMH-1 Cited
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DMH-1 is a potent and selective Bone Morphogenetic Protein (BMP) inhibitor.
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CitedALK-IN-1
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ALK-IN-1 (AP26113) is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.
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SB-431542 Cited
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SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.
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CitedAlectinib hydrochloride
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LDN-193189 2HCl
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LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.
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CitedSelect Batch
Purity:98.23%
Contact us for more batch information
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours. |
| Targets&IC50 | TGFβRI:47 nM, BMPR1A:40 μM (Kd), ALK1:7.1 μM (Kd), ALK5:0.74 μM (Kd), ALK6:0.017 μM (Kd), ACVR1:6.2 μM (Kd), ALK4:1 μM (Kd) |
| In vitro | Inhibiting ligand-activated SMAD3/4 transcription, AZ12799734[2]. AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[2]. AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[2]. |
| In vivo | Inducing histopathologic heart valve lesions in rats, AZ12799734 is administered orally at doses ranging from 0 to 400 mg/kg/day for 3-7 days[1]. At a single oral dose of 50 mg/kg, AZ12799734 shows total and free pharmacokinetic (PK) levels in nude mice over time, exceeding the in vitro IC50 of 0.01885 μM[2]. |
| Alias | AZ12799734 |
| Molecular Weight | 370.43 |
| Formula | C18H18N4O3S |
| Cas No. | 1117684-36-2 |
| Smiles | O(C=1C=C(NC2=CC=C(S(N)(=O)=O)C=C2)N=CC1)C3=C(C)N=C(C)C=C3 |
Storage & Solubility Information
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (215.97 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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