Ceralasertib (AZD6738)

製品コードS7693 バッチS769307

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

C₂₀H₂₄N₆O₂S

分子量

412.51

CAS No.

1352226-88-0

Solubility (25°C)*

体外

DMSO

83 mg/mL (201.2 mM)

Ethanol (warmed with 50ºC water bath)

2 mg/mL (4.84 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	Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
in vitro	Ceralasertib (AZD6738) inhibits ATR kinase activity and impairs cell viability in four Kras mutant cell lines: H23, H460, A549, and H358. In ATM-deficient H23 cells, it strongly synergizes with NSC 119875 to induce rapid cell death. ^[1] In p53 or ATM defective cells, this compound treatment results in replication fork stalls and accumulation of unrepaired DNA damage, resulting in cell death by mitotic catastrophe. ^[2]
in vivo	In nude mice bearing H460 and H23 tumors, Ceralasertib (AZD6738) (50 mg/kg, p.o.) results in tumor growth inhibition (TGI), and its combination with NSC 119875 causes rapid regression of ATM-deficient H23 tumors. ^[1] In nude mice bearing LoVo xenografts, this compound (50 mg/kg) + IR (2 Gy) avoids toxicity while still maintaining efficacy. ^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	H23, H460, A549, and H358 cells
	濃度	~30 μM
	反応時間	48 h
	実験の流れ	Cells are treated in white walled, clear bottom 96-well plates with the indicated doses of Ceralasertib (AZD6738), NSC 119875, LY-188011, or combination for 48 h. ATP levels are assessed as surrogate measure of viability is assessed using the CellTiter-Glo Luminescent Cell Viability Assay and Safire2 plate reader. Raw data are corrected for background luminescence prior to further analysis. For this compound, log dose response curves are generated in GraphPad Prism 6 by nonlinear regression (log(inhibitor) vs. response with variable slope) of log-transformed (x = log(x)) data normalized to the mean of untreated controls. GI50 values, defined as the dose X at which Y = 50%, were extrapolated from dose response curves.
動物実験	動物モデル	Female athymic nude mice bearing H23 or H460 xenografts
	投薬量	25 or 50 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/26517239/
https://pubmed.ncbi.nlm.nih.gov/26312880/
https://pubmed.ncbi.nlm.nih.gov/26310312/

カスタマーフィードバック

: Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1346]

: Data from [Data independently produced by , , J Exp Clin Cancer Res, 2018, 37(1):205]

: Data from [Data independently produced by , , Sci Rep, 2017, 7:41950]

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：

KEAP1 and STK11/LKB1 alterations enhance vulnerability to ATR inhibition in KRAS mutant non-small cell lung cancer [ Cancer Cell, 2025, 43(8):1530-1548.e9]	PubMed: 40645185
Chromosome mis-segregation triggers cell cycle arrest through a mechanosensitive nuclear envelope checkpoint [ Nat Cell Biol, 2025, 27(1):73-86]	PubMed: 39779939
EXO1 as a therapeutic target for Fanconi Anaemia, ZRSR2 and BRCA1-A complex deficient cancers [ Nat Commun, 2025, 16(1):8476]	PubMed: 41006228
WNK1-dependent water influx is required for CD4+ T cell activation and T cell-dependent antibody responses [ Nat Commun, 2025, 16(1):1857]	PubMed: 39984435
KLF5 loss sensitizes cells to ATR inhibition and is synthetic lethal with ARID1A deficiency [ Nat Commun, 2025, 16(1):480]	PubMed: 39779698
CHD6 has poly(ADP-ribose)- and DNA-binding domains and regulates PARP1/2-trapping inhibitor sensitivity via abasic site repair [ Nat Commun, 2025, 16(1):1026]	PubMed: 39863586
The DNA replication checkpoint prevents PCNA/RFC depletion to protect forks from HLTF-induced collapse in human cells [ Mol Cell, 2025, 85(13):2474-2486.e6]	PubMed: 40578346
USP37 counteracts HLTF to protect damaged replication forks and promote survival of BRCA1-deficient cells and PARP inhibitor resistance [ Nucleic Acids Res, 2025, 53(12)gkaf544]	PubMed: 40548939
WIP1 mutations suppress DNA damage triggered bypass of the mitotic timer [ EMBO J, 2025, 10.1038/s44318-025-00495-0]	PubMed: 40551011
Gemcitabine and ATR inhibitors synergize to kill PDAC cells by blocking DNA damage response [ Mol Syst Biol, 2025, 21(3):231-253]	PubMed: 39838187

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。