AZD4573

製品コードS8719 バッチS871901

印刷

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

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.000mg/ml (9.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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, this compound 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, this compound 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 this compound.
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

http://cancerres.aacrjournals.org/content/78/13_Supplement/1650
http://cancerres.aacrjournals.org/content/78/13_Supplement/310
https://pubmed.ncbi.nlm.nih.gov/36026503/

https://pubmed.ncbi.nlm.nih.gov/33306391/

+ 展开

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：

A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8]	PubMed: 40147445
The Polybrominated Diphenyl Ether Bromoxib Disrupts Nuclear Import and Export by Affecting Nucleoporins of the Nuclear Pore Complex [ Mar Drugs, 2025, 23(3)108]	PubMed: 40137294
Inherited blood cancer predisposition through altered transcription elongation [ Cell, 2024, 187(3):642-658.e19]	PubMed: 38218188
Inherited blood cancer predisposition through altered transcription elongation [ Cell, 2024, 187(3):642-658.e19]	PubMed: 38218188
CRL3ARMC5 ubiquitin ligase and Integrator phosphatase form parallel mechanisms to control early stages of RNA Pol II transcription [ Mol Cell, 2024, 84(24):4808-4823.e13]	PubMed: 39667934
High iASPP (PPP1R13L) expression is an independent predictor of adverse clinical outcome in acute myeloid leukemia (AML) [ Cell Death Dis, 2024, 15(11):869]	PubMed: 39616159
Wogonin protects against bleomycin-induced mouse pulmonary fibrosis via the inhibition of CDK9/p53-mediated cell senescence [ Front Pharmacol, 2024, 15:1407891]	PubMed: 39040475
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
Large language models completely understand molecular characteristics of squamous cervical cancer [ Research Square, 2023, Version 1]	PubMed: None
Nuclear microRNAs release paused Pol II via the DDX21-CDK9 complex [ Cell Rep, 2022, 39(2):110673]	PubMed: 35417682

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。