| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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
() |
| [storage]
Store at -20°C | [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 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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