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Purity: ≥98%
AZD3229 (AZD-3229) is a novel, potent, pan-KIT mutant inhibitor with anticancer activity. It has the potential to treat gastrointestinal stromal tumors and shows low nanomolar growth inhibition against a variety of mutant KIT-driven Ba/F3 cell lines (GI50=1–50 nM), with a good margin to KDR-driven effects. Additionally, it suppresses Tel-PDGFRα, Tel-PDGFRβ, and V561D/D842V PDGFR mutants. In addition, it exhibits strong pharmacodynamic inhibition of the target, good cross-species pharmacokinetics, and activity in multiple in vivo models of GIST. Its kinome selectivity is comparable to the best of the approved GIST agents, and its selectivity over KDR can be primarily explained by the interaction of water molecules with the protein and ligand in the active site.
| Targets |
Kit; PDGFRα; PDGFRβ
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|---|---|
| ln Vitro |
With growth inhibitory effects on a range of mutant KIT-driven Ba/F3 cell lines (GI50=1–50 nM), AZD3229 is a powerful mutant KIT mutant [1].
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| ln Vivo |
In mice, rats, and dogs, bioavailability is high and clearance is low in preclinical species. Low distribution volume is consistent with the neutral structure [1]. Tumor volume regression is more successfully induced by AZD3229 at a dose of 20 mg/kg b.i.d. in in vivo models using Ba/F3 cell lines than by imatinib and regorafenib at a dose of 100 mg/kg q.d.[2].
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| References |
[1]. Ryu H, et.al. Antitumor Activity of a Novel Tyrosine Kinase Inhibitor AIU2001 Due to Abrogation of the DNA Damage Repair in Non-Small Cell Lung Cancer Cells. Int J Mol Sci. 2019 Sep 24;20(19):4728.
[2]. Kettle JG, et al. Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy) quinazolin-4-yl]amino} phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. J Med Chem. 2018 Oct 11;61(19):8797-8810. |
| Molecular Formula |
C24H26FN7O3
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|---|---|
| Molecular Weight |
479.506747722626
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| Exact Mass |
479.21
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| Elemental Analysis |
C, 60.12; H, 5.47; F, 3.96; N, 20.45; O, 10.01
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| CAS # |
2248003-60-1
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| Related CAS # |
AZD3229 Tosylate;2248003-71-4
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| Appearance |
Solid powder
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| SMILES |
CC(C)C1=CN(N=N1)CC(=O)NC2=CC=C(C=C2)NC3=NC=NC4=C3C(=CC(=C4)OCCOC)F
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| InChi Key |
FLJOFQUXYAWOPE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26FN7O3/c1-15(2)21-12-32(31-30-21)13-22(33)28-16-4-6-17(7-5-16)29-24-23-19(25)10-18(35-9-8-34-3)11-20(23)26-14-27-24/h4-7,10-12,14-15H,8-9,13H2,1-3H3,(H,28,33)(H,26,27,29))
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| Chemical Name |
N-[4-[[5-fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino]phenyl]-2-(4-propan-2-yltriazol-1-yl)acetamide
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| Synonyms |
AZD3229; AZD 3229; AZD-3229
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| HS Tariff Code |
2934.99.03.00
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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: 40~96 mg/mL (83.4~200.2 mM)
Ethanol: ˂1 mg/mL Water: ˂1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 4 mg/mL (8.34 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 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: 4 mg/mL (8.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 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: 4 mg/mL (8.34 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0855 mL | 10.4273 mL | 20.8546 mL | |
| 5 mM | 0.4171 mL | 2.0855 mL | 4.1709 mL | |
| 10 mM | 0.2085 mL | 1.0427 mL | 2.0855 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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