- AZD3229
-
- $37.00
-
2026-07-27
- CAS:2248003-60-1
- Purity: 99.46%
- Supply Ability: 10g
|
| | AZD3229 Basic information |
| Product Name: | AZD3229 | | Synonyms: | AZD3229;AZD3229
(AZD-3229;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)-;AZD3229, 10 mM in DMSO;NB-003 | | CAS: | 2248003-60-1 | | MF: | C24H26FN7O3 | | MW: | 479.51 | | EINECS: | | | Product Categories: | | | Mol File: | 2248003-60-1.mol |  |
| | AZD3229 Chemical Properties |
| 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 |
| | AZD3229 Usage And Synthesis |
| 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 |
|