AZ32

製品コードS8729 バッチS872901

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₀H₁₆N₄O
	分子量	328.37	CAS No.	2288709-96-4
Solubility (25°C)*	体外	DMSO	66 mg/mL (200.99 mM)
		Ethanol	7 mg/mL (21.31 mM)
		Water	Insoluble
* <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	AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.
in vitro	AZ32 blocks the DNA damage response (DDR) and radiosensitized GBM cells in vitro. AZ32 shows moderate potency against ATM in cell (IC50 = 0.31 μM) and adequate selectivity over ATR, while also having high cell permeability^[1].
in vivo	AZ32, with enhanced blood-brain barrier (BBB) penetration, was highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. AZ32 is the first ATMi with oral bioavailability shown to radiosensitize glioma and improve survival in orthotopic mouse models. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free brain concentrations of AZ32 was in excess of the cellular IC50 for approximately 22 hr. AZ32 has enhanced BBB penetration at 8.7-fold and improved brain coverage over AZ31 but with reduced ATM selectivity^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	U1242 cells
	濃度	3 μM
	反応時間	48 h
	実験の流れ	Human glioma U1242 cells were treated with AZ32 (3 μM) and radiation (2 Gy) or left untreated. At 48 hrs the cells were fixed and processed for ICC using anti-γ-tubulin (centrosomes) and -α-tubulin (microtubules). Cells were counterstained with DAPI to visualize nuclei.
動物実験	動物モデル	orthotopic GL261 glioma model (GL261/luc-red cells intracranially injected into C57bl6 mice)
	投薬量	200 mg/kg
	投与方法	p.o.

参考

[1] Karlin J, et al. Mol Cancer Ther. 2018, 17(8):1637-1647.

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：

Sensitization of Patient-Derived Colorectal Cancer Organoids to Photon and Proton Radiation by Targeting DNA Damage Response Mechanisms [ Cancers (Basel), 2022, 14(20)4984]	PubMed: 36291768

Sensitization of Patient-Derived Colorectal Cancer Organoids to Photon and Proton Radiation by Targeting DNA Damage Response Mechanisms [ Cancers (Basel), 2022, 14(20)4984]

PubMed: 36291768

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。

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