AZD3229
- Product Name
- AZD3229
- CAS No.
- 2248003-60-1
- Chemical Name
- AZD3229
- Synonyms
- NB-003;AZD3229;AZD3229 (AZD-3229;AZD3229, 10 mM in DMSO;AZD3229;AZD 3229;AZD-3229;Inhibitor,AZD3229,CD117,AZD 3229,AZD-3229,SCFR,c-Kit,inhibit;1H-1,2,3-Triazole-1-acetamide, N-[4-[[5-fluoro-7-(2-methoxyethoxy)-4-quinazolinyl]amino]phenyl]-4-(1-methylethyl)-
- CBNumber
- CB04667591
- Molecular Formula
- C24H26FN7O3
- Formula Weight
- 479.51
- MOL File
- 2248003-60-1.mol
AZD3229 Property
- Density
- 1.35±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:68.67(Max Conc. mg/mL);143.21(Max Conc. mM)
DMF:10.0(Max Conc. mg/mL);20.85(Max Conc. mM)
Ethanol:0.3(Max Conc. mg/mL);0.63(Max Conc. mM) - form
- A crystalline solid
- pka
- 12.75±0.70(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 27908
- Product name
- AZD 3229
- Packaging
- 500μg
- Price
- $68
- Updated
- 2024/03/01
- Product number
- 27908
- Product name
- AZD 3229
- Packaging
- 5mg
- Price
- $286
- Updated
- 2024/03/01
- Product number
- 27908
- Product name
- AZD 3229
- Packaging
- 1mg
- Price
- $130
- Updated
- 2024/03/01
- Product number
- CS-0065717
- Product name
- AZD3229
- Purity
- 99.55%
- Packaging
- 5mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- orb573321
- Product name
- AZD3229
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1949.9
- Updated
- 2021/12/16
AZD3229 Chemical Properties,Usage,Production
Uses
AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC50 value of 223.3 nM[1][2].
Biological Activity
AZD3229 is a potent pan-Kit (c-Kit) mutant inhibitor with GI50 of 1-50 nM in a Kit (c-Kit) mutant-driven Ba/F3 cell line. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).
in vivo
AZD3229 has high bioavailability, low clearance and small volume of distribution in preclinical animal models of mice, rats and dogs. In an in vivo model constructed using the Ba/F3 cell line, AZD3229 at 20 mg/kg bid induces regression of tumor volume more effectively than regorafenib and imatinib at 100 mg/kg qd.
target
| Target | Value |
| Kit () | |
| PDGFRα () | |
| PDGFRβ () |
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. DOI:10.3390/ijms20194728
[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. DOI:10.1021/acs.jmedchem.8b00938
AZD3229 Preparation Products And Raw materials
Raw materials
Preparation Products
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