Ceralasertib (AZD6738)

製品コードS7693 バッチS769305

印刷

化学情報

Chemical Structure 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) 83 mg/mL (201.2 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO Corn oil
1.88mg/ml Taking the 1 mL working solution as an example, add 50 μL of 37.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
in vitro In four Kras mutant cell lines: H23, H460, A549, and H358, AZD6738 inhibits ATR kinase activity and impairs cell viability. In ATM-deficient H23 cells, AZD6738 strongly synergizes with cisplatin to induce rapid cell death. [1] In p53 or ATM defective cells, AZD6738 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, AZD6738 (50 mg/kg, p.o.) results in tumor growth inhibition (TGI), and the the combination with cisplatin causes rapid regression of ATM-deficient H23 tumors. [1] In nude mice bearing LoVo xenografts, a combination of AZD6738 (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 AZD6738, cisplatin, gemcitabine, 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 AZD6738 treatment, 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.

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：

Functionally-instructed modifiers of response to ATR inhibition in experimental glioma [ J Exp Clin Cancer Res, 2024, 43(1):77] PubMed: 38475864
MGMT function determines the differential response of ATR inhibitors with DNA-damaging agents in glioma stem cells for GBM therapy [ Neurooncol Adv, 2024, 6(1):vdad165] PubMed: 38213834
C16orf72/HAPSTR1/TAPR1 functions with BRCA1/Senataxin to modulate replication-associated R-loops and confer resistance to PARP disruption [ Nat Commun, 2023, 14(1):5003] PubMed: 37591890
"Proteotranscriptomic analysis of advanced colorectal cancer patient derived organoids for drug sensitivity prediction" [ J Exp Clin Cancer Res, 2023, 42(1):8] PubMed: 36604765
Irreversible HER2 inhibitors overcome resistance to the RSL3 ferroptosis inducer in non-HER2 amplified luminal breast cancer [ Cell Death Dis, 2023, 14(8):532] PubMed: 37596261
DNA damage response inhibitors enhance tumour treating fields -TTFields) potency in glioma stem-like cells [ Br J Cancer, 2023, 10.1038/s41416-023-02454-0] PubMed: 37777579
Mitotic perturbation is a key mechanism of action of decitabine in myeloid tumor treatment [ Cell Rep, 2023, 42(9):113098] PubMed: 37714156
ATR protects ongoing and newly assembled DNA replication forks through distinct mechanisms [ Cell Rep, 2023, 42(7):112792] PubMed: 37454295
Effector memory T cells induce innate inflammation by triggering DNA damage and a non-canonical STING pathway in dendritic cells [ Cell Rep, 2023, S2211-1247(23)01192-0] PubMed: 37794597
Immunogenic cell death after combined treatment with radiation and ATR inhibitors is dually regulated by apoptotic caspases [ Front Immunol, 2023, 14:1138920] PubMed: 37346039

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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