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. This compound also inhibits the cell proliferation, decreases cell viability and elicits the caspase 3/7 activity in Colo-205 cells. Moreover, it 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 this compound 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/22560567/

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：

DNA polymerase α/primase extraction from chromatin by VCP/p97 restricts ATR activation during unperturbed DNA replication [ Nat Commun, 2025, 16(1):5706] PubMed: 40593507
Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9] PubMed: 40449480
Quantitative Chromatin Protein Dynamics During Replication Origin Firing in Human Cells [ Mol Cell Proteomics, 2025, 24(3):100915] PubMed: 39880081
Identifying TP53RK as a key regulator of colorectal cancer survival and a potential therapeutic target [ Sci Rep, 2025, 15(1):36122] PubMed: 41102525
Enhancing transcription-replication conflict targets ecDNA-positive cancers [ Nature, 2024, 635(8037):210-218] PubMed: 39506153
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

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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