| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
AZ-23 targets TrkA, TrkB, and TrkC (tropomyosin receptor kinases) with IC50 values of 2 nM, 8 nM, and 24 nM, respectively. It is an ATP-competitive inhibitor. It also inhibits FGFR1 (24 nM), Flt3 (52 nM), Ret (55 nM), MuSk (84 nM), and Lck (99 nM). These kinases are involved in cell proliferation, survival, and differentiation.
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| ln Vitro |
In cells, AZ-23 strongly and specifically suppresses Trk phosphorylation. With an EC50 of 2 nM, AZ-23 potently suppresses Trk-mediated survival. TF-1 and MCF10ATrkA-Δ cell lines' Trk-dependent survival is inhibited by AZ-23 [1].
In vitro, AZ-23 potently inhibits TrkA with an IC50 of 2 nM, TrkB with an IC50 of 8 nM, and TrkC with an IC50 of 24 nM. It also inhibits FGFR1 (24 nM), Flt3 (52 nM), Ret (55 nM), MuSk (84 nM), and Lck (99 nM). It is an ATP-competitive inhibitor. These activities contribute to its potential anticancer effects. |
| ln Vivo |
In a TrkA-driven allograft model, AZ-23 shows efficacious inhibitory effects on TrkA kinase in mice after oral administration; in a Trk-expressing neuroblastoma xenograft model, the drug significantly inhibits tumor growth[1].
In vivo, AZ-23 is orally bioavailable. It has been studied in animal models of cancer where Trk signaling is dysregulated. By inhibiting Trk kinases, it disrupts tumor cell proliferation and survival. Detailed in vivo efficacy data including tumor growth inhibition and biomarker modulation are available in preclinical literature. |
| Enzyme Assay |
In vitro kinase assays for AZ-23 typically involve measuring the inhibition of recombinant TrkA, TrkB, and TrkC kinases using radiometric or fluorescence-based methods. The kinase is incubated with a substrate (e.g., a peptide or protein) and ATP in the presence of varying concentrations of the compound. IC50 values are calculated from dose-response curves. Selectivity is assessed by screening against a panel of kinases.
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| Cell Assay |
Cell-based assays for AZ-23 involve culturing cancer cell lines that are dependent on Trk signaling for growth and survival. Cells are treated with AZ-23 at concentrations ranging from 0.1 nM to 10 µM for 24-72 hours. Cell viability is assessed by MTT or CellTiter-Glo assays. Trk phosphorylation is measured by Western blot using phospho-specific antibodies. Apoptosis is evaluated by flow cytometry.
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| Animal Protocol |
In vivo animal experiments for AZ-23 typically involve administration to tumor-bearing mice (xenograft models) via oral gavage. Tumor growth inhibition is monitored. Trk phosphorylation in tumor tissues is assessed by Western blot or immunohistochemistry. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues. Toxicity is assessed by monitoring body weight and organ histology.
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| ADME/Pharmacokinetics |
AZ-23 (molecular weight 391.83, formula C21H20ClN5O) is orally bioavailable. It is soluble in DMSO at 90 mg/mL. Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature. Its favorable oral bioavailability supports its use in in vivo studies.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for AZ-23 from the search results. As a Trk kinase inhibitor, potential toxicity may include effects on nervous system function where Trk signaling is important. Comprehensive toxicological evaluation including acute, subchronic, and genotoxicity studies has likely been conducted in preclinical development. The compound is for research use only.
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| References | |
| Additional Infomation |
AZ-23 (CAS#: 915720-21-7) is an ATP-competitive, orally bioavailable TrkA/B/C inhibitor with IC50 values of 2 nM, 8 nM, and 24 nM, respectively. It also inhibits FGFR1, Flt3, Ret, MuSk, and Lck. It is used in cancer research. Molecular weight: 391.83, formula: C21H20ClN5O.
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| Molecular Formula |
C17H19CLFN7O
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|---|---|
| Molecular Weight |
391.830464601517
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| Exact Mass |
391.132
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| CAS # |
915720-21-7
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| PubChem CID |
16097523
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
596.1±60.0 °C at 760 mmHg
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| Flash Point |
314.3±32.9 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.655
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| LogP |
2.64
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
463
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H](C1=NC=C(C=C1)F)NC2=NC=C(C(=N2)NC3=CC(=NN3)OC(C)C)Cl
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| InChi Key |
LBVKEEFIPBQIMD-JTQLQIEISA-N
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| InChi Code |
InChI=1S/C17H19ClFN7O/c1-9(2)27-15-6-14(25-26-15)23-16-12(18)8-21-17(24-16)22-10(3)13-5-4-11(19)7-20-13/h4-10H,1-3H3,(H3,21,22,23,24,25,26)/t10-/m0/s1
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| Chemical Name |
5-chloro-2-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-4-N-(3-propan-2-yloxy-1H-pyrazol-5-yl)pyrimidine-2,4-diamine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~319.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5521 mL | 12.7606 mL | 25.5213 mL | |
| 5 mM | 0.5104 mL | 2.5521 mL | 5.1043 mL | |
| 10 mM | 0.2552 mL | 1.2761 mL | 2.5521 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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