AZD7648

製品コードS8843 バッチS884301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₈H₂₀N₈O₂

分子量

380.40

CAS No.

2230820-11-6

Solubility (25°C)*

体外

DMSO

6 mg/mL (15.77 mM)

Water

Insoluble

Ethanol

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	AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases.
in vitro	AZD7648 inhibits IR-induced DNA-PK S2056 auto phosphoryalation with an IC50 = 92 nM in A549 non-small cell lung cancer (NSCLC) cells. In A549 cells, this compound (≥1 µM) in combination with 2Gy IR for 48 hours leads to a significant accumulation of cells arrested in the G2/M of the cell cycle, a 4-fold increase in micronuclei formation, and 3-fold induction of γH2AX, pATM S1981 and 53BP1 foci formation compared with IR alone^[2].
in vivo	AZD7648 is a potent and highly selective DNA-PK inhibitor, with good crystalline solubility, permeability and metabolic stability, good bioavailability and predictable pharmacokinetics in preclinical species, and potent knockdown of pRPA and regressions in murine xenograft models when combining with AZD2281 or radiation^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HeLa cells
	濃度	10 μM
	反応時間	1 h
	実験の流れ	Cells were treated with indicated concentration of this compound for 1 h.
動物実験	動物モデル	SCID mice
	投薬量	4-100 mg/kg
	投与方法	p.o.

参考

https://cancerres.aacrjournals.org/content/79/13_Supplement/DDT01-02
https://cancerres.aacrjournals.org/content/79/13_Supplement/3512
https://pubmed.ncbi.nlm.nih.gov/35869071/

https://pubmed.ncbi.nlm.nih.gov/31699977/

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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：

Multilayered HIV-1 resistance in HSPCs through CCR5 Knockout and B cell secretion of HIV-inhibiting antibodies [ Nat Commun, 2025, 16(1):3103]	PubMed: 40164595
Engineering synthetic signaling receptors to enable erythropoietin-free erythropoiesis [ Nat Commun, 2025, 16(1):1140]	PubMed: 39880867
Targeting synthetic lethality between non-homologous end joining and radiation in very-high-risk medulloblastoma [ Cell Rep Med, 2025, 6(7):102202]	PubMed: 40562042
A CRISPR-Cas9 screen reveals genetic determinants of the cellular response to decitabine [ EMBO Rep, 2025, 10.1038/s44319-025-00385-w]	PubMed: 39930152
Bioluminescence-based assays for quantifying endogenous protein interactions in live cells [ J Biol Chem, 2025, 301(8):110454]	PubMed: 40617353
TOX High-Mobility Group Box Family Member 4 promotes DNA double-strand break repair via nonhomologous end joining [ J Biol Chem, 2025, 301(6):110174]	PubMed: 40328361
The aflatoxin B1-induced formamidopyrimidine adduct is repaired by transcription-coupled nucleotide excision repair in human cells [ NAR Cancer, 2025, 7(3):zcaf030]	PubMed: 40918649
Autologous genome-edited hematopoietic stem cells correct Gaucher disease and establish a platform for clinical translation [ Res Sq, 2025, rs.3.rs-7123212]	PubMed: 40894035
Genome editing with the HDR-enhancing DNA-PKcs inhibitor AZD7648 causes large-scale genomic alterations [ Nat Biotechnol, 2024, 10.1038/s41587-024-02488-6]	PubMed: 39604565
Enhancement of erythropoietic output by Cas9-mediated insertion of a natural variant in haematopoietic stem and progenitor cells [ Nat Biomed Eng, 2024, 10.1038/s41551-024-01222-6]	PubMed: 38886504

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。