AZD4573

製品コードS8719 バッチS871902

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₂H₂₈ClN₅O₂
	分子量	429.94	CAS No.	2057509-72-3
Solubility (25°C)*	体外	DMSO	86 mg/mL (200.02 mM)
		Ethanol	86 mg/mL (200.02 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	AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t_1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.
in vitro	Short-term treatment with AZD4573 leads to a rapid dose- and time-dependent decrease in cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines (e.g. caspase activation EC50 0.0137 μM in an acute myeloid leukemia model MV4-11)^[1]. In human cancer cell line panel screens, AZD4573 demonstrates the ability to induce rapid caspase activation (6h) and loss of viability (24h) across a diverse set of hematological cancers (median caspase EC50 = 30 nM, GI50 = 11 nM) but with minimal effect on solid tumors (median EC50 & GI50 >30 μM)^[2].
in vivo	AZD4573 exhibits a short half-life in multiple preclinical species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration^[1].

製品説明

AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t_1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.

in vitro

Short-term treatment with AZD4573 leads to a rapid dose- and time-dependent decrease in cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines (e.g. caspase activation EC50 0.0137 μM in an acute myeloid leukemia model MV4-11)^[1].

In human cancer cell line panel screens, AZD4573 demonstrates the ability to induce rapid caspase activation (6h) and loss of viability (24h) across a diverse set of hematological cancers (median caspase EC50 = 30 nM, GI50 = 11 nM) but with minimal effect on solid tumors (median EC50 & GI50 >30 μM)^[2].

in vivo

AZD4573 exhibits a short half-life in multiple preclinical species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	SLK cells
	濃度	30 nM
	反応時間	8 h
	実験の流れ	Cells were treated with indicated concentrations of drug.
動物実験	動物モデル	Nomo-1 AML xenograft
	投薬量	5 mg/kg
	投与方法	i.p.

参考

[4] Barlaam B, et al. J Med Chem. 2020 Dec 24;63(24):15564-15590.

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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：

Inherited blood cancer predisposition through altered transcription elongation [ Cell, 2024, 187(3):642-658.e19]	PubMed: 38218188
Comprehensive molecular characterization of adenoid cystic carcinoma reveals tumor suppressors as novel drivers and prognostic biomarkers [ J Pathol, 2023, 261(3):256-268]	PubMed: 37565350
Nuclear microRNAs release paused Pol II via the DDX21-CDK9 complex [ Cell Rep, 2022, 39(2):110673]	PubMed: 35417682
PRC1-independent binding and activity of RYBP on the KSHV genome during de novo infection [ PLoS Pathog, 2022, 18(8):e1010801]	PubMed: 36026503
Proteomics and phosphoproteomics of chordoma biopsies reveal alterations in multiple pathways and aberrant kinases activities [ Front Oncol, 2022, 12:941046]	PubMed: 36248973
KAP1 is a new non-genetic vulnerability of malignant pleural mesothelioma (MPM) [ NAR Cancer, 2022, 4(3):zcac024]	PubMed: 35910692
CDK9 Inhibitor Induces the Apoptosis of B-Cell Acute Lymphocytic Leukemia by Inhibiting c-Myc-Mediated Glycolytic Metabolism [ Front Cell Dev Biol, 2021, 9:641271]	PubMed: 33748130
Inhibitors Targeting CDK9 Show High Efficacy against Osimertinib and AMG510 Resistant Lung Adenocarcinoma Cells [ Cancers (Basel), 2021, 13(15)3906]	PubMed: 34359807
Reduced Mitochondrial Apoptotic Priming Drives Resistance to BH3 Mimetics in Acute Myeloid Leukemia [ Cancer Cell, 2020, 38(6):872-890.e6]	PubMed: 33217342
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors [ Cell Chem Biol, 2020, S2451-9456(20)30380-9]	PubMed: 33086052

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。