XL413
Based on 7 publication(s) in Google Scholar
XL413 is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
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
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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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]
- 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.
Customer Validation & Images
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WB
Biological Activity
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Cdc7 3.4 nM (IC50) |
PIM1 42 nM (IC50) |
CK2 215 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| 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] |
XL413 inhibits the cell proliferation (IC50 = 2685 nM), decreases cell viability (IC50 = 2142 nM) and elicits the caspase 3/7 activity (EC50 = 2288 nM) in Colo-205 cells. XL413 also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC50 = 715 nM)[1]. XL413 shows cytotoxic effects on tumors, with IC50 of 22.9 µM in HCC1954 cells and 1.1 µM in Colo-205 cells. XL413 induces apoptosis in the Colo-205 cells, but not in HCC1954 cells. XL413 is effective DDK inhibitors in vitro, with IC50 of 22.7 nM. XL413 is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 (7)
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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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Solvent & Solubility
DMSO : 3.45 mg/mL (11.91 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.35 mg/mL (1.21 mM); Clear solution
This protocol yields a clear solution of ≥ 0.35 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.34 mg/mL (1.17 mM); Clear solution
This protocol yields a clear solution of ≥ 0.34 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.4 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 µCi (γ)-32P ATP and 1.5 µM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC50 values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 µL of this suspension is mixed with 30 µL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 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
[1]. Koltun ES, et al. Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. [Content Brief]
[2]. 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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4516 mL | 17.2580 mL | 34.5161 mL | 86.2902 mL |
| 5 mM | 0.6903 mL | 3.4516 mL | 6.9032 mL | 17.2580 mL | |
| 10 mM | 0.3452 mL | 1.7258 mL | 3.4516 mL | 8.6290 mL |
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