XL413
Based on 8 publication(s) in Google Scholar
XL413 (BMS-863233) is an orally active, ATP-competitive, selective CDC7 kinase inhibitor. XL413 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 attenuates ATR inhibitor-induced excessive origin activation, altered replication fork speed, and antiproliferative effects in sensitive cancer cells. XL413 inhibits SARS-CoV-2 infection. XL413 can be used for research related to cancer and SARS-CoV-2 infection.
For research use only. We do not sell to patients.
- Purity : 99.02%
- CAS No.: 1169558-38-6
- Formula: C14H12ClN3O2
- Molecular Weight:289.72
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) XL413
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
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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 | EC50 |
2288 nM
Compound: 14, XL413
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Induction of apoptosis in human Caco2 cells assessed as increase in caspase 3/7 activity
Induction of apoptosis in human Caco2 cells assessed as increase in caspase 3/7 activity
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[PMID: 22560567] |
| 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
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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] |
| Caco-2 | IC50 |
715 nM
Compound: 14, XL413
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Antiproliferative activity against human Caco2 cells assessed as inhibition of anchorage-independent growth in soft agar
Antiproliferative activity against human Caco2 cells assessed as inhibition of anchorage-independent growth in soft agar
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[PMID: 22560567] |
In Vitro
XL-413 (1 µM; 1 h) 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) partially rescues ATRi-mediated antiproliferative effects in the sensitive breast cancer cell lines HCC1806 and HCC1569[1].
XL-413 (BMS-863233) exhibits antiviral activity against infectious SARS-CoV-2 in Calu-1 cells and produces cytotoxic effects at higher concentrations[2].
XL-413 shows no detectable modulation of DDX39B-related protein-protein interactions at concentrations of 5 μM and 50 μM in HEK293 cells[2].
XL-413 exhibits potent inhibitory activity against purified recombinant DDK (Cdc7-Dbf4) kinase, with IC50 = 22.7 nM[4].
XL-413 (5 μM; 24-72 h) 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 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 inhibits the expression of the early T cell activation marker CD69 in anti-CD3-stimulated mouse lymphocytes[3].
XL-413 (5 μM; 72 h) 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.
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Cell Line:HCC1806 and HCC1569 breast cancer cells
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Concentration:0.25 µM (co-administered with ATRi)
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Incubation Time:72 h
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Result:Reduced the anti-proliferative effect of ATRi in both HCC1806 and HCC1569 ATRi-sensitive breast cancer cell lines, indicating partial rescue of ATRi sensitivity when origin firing capacity is lowered via CDC7 inhibition.
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Cell Line:HCC1954, HeLa, MDA‑MB‑231, HCC1187, BT‑549, MDA‑MB‑453 and MCF‑7 tumor cell lines
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Concentration:5 μM
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Incubation Time:72 h
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Result:Displayed weak antiproliferative activity against HCC1954, HeLa, MDA‑MB‑231, HCC1187, BT‑549, MDA‑MB‑453 and MCF‑7 tumor cell lines, while it shows strong antiproliferative activity against Colo‑205 tumor cells.
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Cell Line:Colo-205 cells
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Concentration:5 μM
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Incubation Time:0, 24, 48, 72 h
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Result:Abolished DDK-dependent MCM2 phosphorylation in Colo-205 cells, whereas only a slight decrease in MCM2 phosphorylation is observed at 72 h in HCC1954 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1169558-38-6
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Appearance Solid
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Molecular Weight 289.72
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Formula C14H12ClN3O2
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Color Off-white to light yellow
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SMILES
ClC1=CC=C2C(C(N=C([C@@H]3CCCN3)NC4=O)=C4O2)=C1
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Synonyms
BMS-863233
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 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
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Data Sheet (284 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
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)