AZD2932

製品コードS7003 バッチS700301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₄H₂₅N₅O₄

分子量

447.49

CAS No.

883986-34-3

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

89 mg/mL (198.88 mM)

Ethanol (warmed with 50ºC water bath)

5 mg/mL (11.17 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
in vitro	AZD2932 effectively inhibits the activities of VEGFR-2 (IC50, 8 nM), PDGFRβ (IC50,4 nM), Flt-3 (IC50, 7 nM), and c-Kit (IC50, 9 nM). This compound inhibits both PDGFRα and PDGFRβ phosphorylation with a correlation close to 1:1. It does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). It has no activity against hERG (IC50, 137 μM).^[1]
in vivo	In C6 rat glial tumor model, AZD2932 (p.o., b.i.d.) results in signiﬁcant TGI of 64% for both 50 and 12.5 mg/kg doses. Growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. (p.o.) and LoVo tumors by 67% at 50 mg/kg b.i.d (p.o.). This compound (3–50 mg/kg, p.o.) causes 60–80% inhibition of both p-VEGFR-2 and p-PDGFRβ. Single bolus oral doses of this chemical results in dose-related inhibition of PDGFRa phosphorylation 6 h after dosing.^[1]

プロトコル(参考用のみ)

動物実験	動物モデル	Nude mice bearing C6 rat glial tumors
	投薬量	50 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/22153662/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Activation of receptor tyrosine kinases mediates acquired resistance to MEK inhibition in malignant peripheral nerve sheath tumors [ Cancer Res, 2020, canres.1992.2020]	PubMed: 33203698
Synergistic Anti Leukemia Effect of a Novel Hsp90 and a Pan Cyclin Dependent Kinase Inhibitors. [ Molecules, 2020, 8;25(9) pii: E2220]	PubMed: 32397330
Contribution of Polycomb group proteins to olfactory basal stem cell self-renewal in a novel c-KIT+ culture model and in vivo. [ Development, 2016, 143(23):4394-4404]	PubMed: 27789621

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。