XL413 hydrochloride
Based on 8 publication(s) in Google Scholar
XL413 hydrochloride (BMS-863233 hydrochloride) is an orally active, ATP-competitive, selective CDC7 kinase inhibitor. XL413 hydrochloride reduces MCM2 phosphorylation levels, decreases DNA replication origin activation, and inhibits CD69 upregulation in stimulated lymphocytes. XL-413 possesses cell-dependent antiproliferative and pro-apoptotic activities. XL413 hydrochloride attenuates ATR inhibitor-induced excessive origin activation, altered replication fork speed, and antiproliferative effects in sensitive cancer cells. XL413 hydrochloride inhibits SARS-CoV-2 infection. XL413 hydrochloride can be used for research related to cancer and SARS-CoV-2 infection.
For research use only. We do not sell to patients.
- CAS No.: 1169562-71-3
- Formula: C14H12ClN3O2.xHCl
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) XL413 hydrochloride
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- MedComm (2020). 2025 May 15;6(6):e70150. [Abstract]
- J Transl Med. 2026 Jul 11.
- Sens Actuators B Chem. 15 May 2022, 131618.
- Oncogenesis. 2026 Apr 24;15(1):27. [Abstract]
- Am J Physiol Lung Cell Mol Physiol. 2018 Sep 1;315(3):L360-L370. [Abstract]
- bioRxiv. 2025 Dec 9.
- University of Washington. 2025.
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WB
All Caspase Isoforms
More
Biological Activity
Description
|
Cdc7 3.4 nM (IC50) |
Caspase 3 |
Caspase-7 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | ED50 |
<3 mg/kg
Compound: 14, XL413
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Inhibition of CDC7-mediated MCM2 phosphorylation at Ser40/41 in human Caco2 cells xenografted in po dosed athymic nude mouse by after 4 hrs Western blot analysis
Inhibition of CDC7-mediated MCM2 phosphorylation at Ser40/41 in human Caco2 cells xenografted in po dosed athymic nude mouse by after 4 hrs Western blot analysis
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[PMID: 22560567] |
| Caco-2 | IC50 |
140 nM
Compound: 14, XL413
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Inhibition of CDC7 in human Caco2 cells assessed as inhibition of MCM2 phosphorylation at Ser53 after 4 hrs
Inhibition of CDC7 in human Caco2 cells assessed as inhibition of MCM2 phosphorylation at Ser53 after 4 hrs
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[PMID: 22560567] |
| Caco-2 | IC50 |
2142 nM
Compound: 14, XL413
|
Antiproliferative activity against human Caco2 cells assessed as decrease in cell viability after 3 days by Cell Titer-Glo assay
Antiproliferative activity against human Caco2 cells assessed as decrease in cell viability after 3 days by Cell Titer-Glo assay
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[PMID: 22560567] |
| Caco-2 | IC50 |
2685 nM
Compound: 14, XL413
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Antiproliferative activity against human Caco2 cells after 3 days by BrdU incorporation assay
Antiproliferative activity against human Caco2 cells after 3 days by BrdU incorporation assay
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[PMID: 22560567] |
In Vitro
XL-413 (1 µM; 1 h) hydrochloride reduces baseline origin activation levels and reverses ATRi-induced alterations in origin density and replication fork speed in HCC1806 breast cancer cells; it decreases EdU incorporation and inhibits ATRi-induced replication origin hyperactivation in HCC1806 breast cancer cells[1].
XL-413 (0.25 µM; 72 h) hydrochloride partially rescues ATRi-mediated antiproliferative effects in the sensitive breast cancer cell lines HCC1806 and HCC1569[1].
XL-413 (BMS-863233) hydrochloride exhibits antiviral activity against infectious SARS-CoV-2 in Calu-1 cells and produces cytotoxic effects at higher concentrations[2].
XL-413 hydrochloride shows no detectable modulation of DDX39B-related protein-protein interactions at concentrations of 5 μM and 50 μM in HEK293 cells[2].
XL-413 hydrochloride exhibits potent inhibitory activity against purified recombinant DDK (Cdc7-Dbf4) kinase, with IC50 = 22.7 nM[4].
XL-413 (5 μM; 24-72 h) hydrochloride abolishes DDK-dependent MCM2 phosphorylation in Colo-205 cells, whereas only a slight decrease in MCM2 phosphorylation is observed at 72 h in HCC1954 cells[4].
XL-413 hydrochloride potently and selectively inhibits CDC7 kinase activity in Jurkat cells and OT-I CTLs; it inhibits CDC7 with an IC50 of 3.4 nM in biochemical assays[3].
XL-413 hydrochloride inhibits the expression of the early T cell activation marker CD69 in anti-CD3-stimulated mouse lymphocytes[3].
XL-413 (5 μM; 72 h) hydrochloride exhibits potent antiproliferative and pro-apoptotic activity against Colo-205 colorectal cancer cells (IC50 = 1.1 μM), but shows weak antiproliferative effects on HCC1954 breast cancer cells (IC50 = 22.9 μM)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1169562-71-3
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Formula C14H12ClN3O2.xHCl
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SMILES
ClC1=CC=C2C(C(N=C([C@@H]3CCCN3)NC4=O)=C4O2)=C1.Cl.[x]
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Synonyms
BMS-863233 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (8)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
MedComm (2020)
2025 May 15;6(6):e70150. PMID: 40384988 -
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Oncogenesis
2026 Apr 24;15(1):27. PMID: 42031714 -
Am J Physiol Lung Cell Mol Physiol
Cell division cycle 7 kinase is a negative regulator of cell-mediated collagen degradation. [Abstract]2018 Sep 1;315(3):L360-L370. PMID: 29792348
XL413 hydrochloride purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2018 Sep 1;315(3):L360-L370. [Abstract]
Representative Western blot for Endo180 expression in U937 cells treated overnight with XL413.
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Purity & Documentation
References
[2]. Liu X, et al. SARS-CoV-2-host proteome interactions for antiviral drug discovery. Molecular systems biology. 2021 Nov;17(11):e10396. [Content Brief]
[3]. Chen EW, et al. A Dual Inhibitor of Cdc7/Cdk9 Potently Suppresses T Cell Activation. Frontiers in immunology. 2019;10:1718. [Content Brief]
[4]. Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e113300. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)