XL413

Catalog No.S7547 Batch:S754702

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Technical Data

Formula

C14H13Cl2N3O2
Molecular Weight 326.18 CAS No. 1169562-71-3
Solubility (25°C)* In vitro Water 40 mg/mL (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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description XL413 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.
Targets
Cdc7 [1]
(Cell-free assay)		 Pim1 [1]
(Cell-free assay)		 CK2 [1]
(Cell-free assay)
3.4 nM 42 nM 212 nM
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]

Protocol (from reference)

Kinase Assay:

[1]
  • 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.
Cell Assay:

[1]
  • Cell lines

    Colo-205 cells

  • Concentrations

    ~10 μM

  • Incubation Time

    24 hours

  • Method

    The cell proliferation is measured by BrdU incorporation assay, and viability is assayed by Cell Titer–Glo kits.
Animal Study:

[1]
  • Animal Models

    Mice bearing Colo-205 xenografts

  • Dosages

    ~100 mg/kg

  • Administration

    p.o.

Customer Product Validation

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's XL413 has been cited by 29 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.