XL413

製品コードS7547 バッチS754702

印刷

化学情報

Chemical Structure Synonyms BMS-863233 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H13Cl2N3O2
分子量 326.18 CAS No. 1169562-71-3
Solubility (25°C)* 体外 Water 40 mg/mL warmed with 50ºC water bath (122.63 mM)
DMSO Insoluble
Ethanol 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 XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2.
in vitro In MDA-MB-231T and Colo-205 cell lines, XL413 results in inhibition of CDC7 specific phosphorylation of MCM2. XL413 also inhibits the cell proliferation, decreases cell viability and elicits the caspase 3/7 activity in Colo-205 cells. Moreover, XL413 results in modified S phase progression that subsequently leads to apoptotic cell death. [1]
in vivo In a Colo-205 xenograft model, XL413, at the 3 mg/kg dose, causes 70% inhibition of phosphorylated MCM2, and causes significant tumor growth regression at the 100 mg/kg dose. [1]

プロトコル(参考用のみ)

キナーゼアッセイ CDC7 kinase assay
Kinase activity and compound inhibition are determined using the luciferase-luciferin-coupled chemiluminescence assay and measured as the percentage of ATP utilized following the kinase reaction in a 384-well format. The final CDC7 kinase assay condition is 6 nM CDC7/ASK, 1 μM ATP, 50 mM Hepes pH 7.4, 10 mM MgCl2, 0.02% BSA, 0.02% brij 35, 0.02% tween 20 and 1 mM DTT. It is worthy to note that the CDC7/ASK protein exhibits substrate-independent ATP utilization. All kinase reactions are incubated at room temperature for 1-2 h.
細胞アッセイ 細胞株 Colo-205 cells
濃度 ~10 μM
反応時間 24 hours
実験の流れ

The cell proliferation is measured by BrdU incorporation assay, and viability is assayed by Cell Titer–Glo kits.
動物実験 動物モデル Mice bearing Colo-205 xenografts
投薬量 ~100 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 , , J Mol Med, 2018, 96(6):513-525]

Data from [Data independently produced by , , Exp Cell Res, 2015, 339(2):289-99.]

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：

Effective sequential combined therapy with carboplatin and a CDC7 inhibitor in ovarian cancer [ Transl Oncol, 2024, 39:101825] PubMed: 37992591
SF3B1 hotspot mutations confer sensitivity to PARP inhibition by eliciting a defective replication stress response [ Nat Genet, 2023, 55(8):1311-1323] PubMed: 37524790
CDC7 inhibition induces replication stress-mediated aneuploid cells with an inflammatory phenotype sensitizing tumors to immune checkpoint blockade [ Nat Commun, 2023, 10.1038/s41467-023-43274-3] PubMed: 37980406
DBF4 Dependent Kinase Inhibition Suppresses Hepatocellular Carcinoma Progression and Potentiates Anti-Programmed Cell Death-1 Therapy [ Int J Biol Sci, 2023, 19(11):3412-3427] PubMed: 37497004
Modulating mutational outcomes and improving precise gene editing at CRISPR-Cas9-induced breaks by chemical inhibition of end-joining pathways [ Cell Rep, 2023, 42(2):112019] PubMed: 36701230
ATR protects ongoing and newly assembled DNA replication forks through distinct mechanisms [ Cell Rep, 2023, 42(7):112792] PubMed: 37454295
Identifying CDC7 as a synergistic target of chemotherapy in resistant small-cell lung cancer via CRISPR/Cas9 screening [ Cell Death Discov, 2023, 9(1):40] PubMed: 36725843
Cancer-associated FBXW7 loss is synthetic lethal with pharmacological targeting of CDC7 [ Mol Oncol, 2023, 10.1002/1878-0261.13537] PubMed: 37866880
A function for ataxia telangiectasia and Rad3-related (ATR-kinase in cytokinetic abscission. [ iScience, 2023, 25(7)] PubMed: None
RAD52 prevents accumulation of Polα-dependent replication gaps at perturbed replication forks in human cells [ bioRxiv, 2023, 2023.04.12.536536] PubMed: 37090680

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。