Home Cell Cycle CDK inhibitor XL413 For research use only.

XL413

Synonyms: BMS-863233

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.

XL413 Chemical Structure

XL413 Chemical Structure

CAS No. 1169562-71-3

Purity & Quality Control

XL413 Related Products

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231T cells Function assay 4 h Inhibition of CDC7 in human MDA-MB-231T cells assessed as inhibition of MCM2 phosphorylation at Ser53 after 4 hrs, IC50=0.118 μM 22560567
human Caco2 cells Function assay 4 h Inhibition of CDC7 in human Caco2 cells assessed as inhibition of MCM2 phosphorylation at Ser53 after 4 hrs, IC50=0.14 μM 22560567
human Caco2 cells Proliferation assay Antiproliferative activity against human Caco2 cells assessed as inhibition of anchorage-independent growth in soft agar, IC50=0.715 μM 22560567
Caco2 cells Function assay Induction of apoptosis in human Caco2 cells assessed as increase in caspase 3/7 activity, EC50=2.288 μM 22560567
MDA-MB-468 Function assay Inhibition of PHGDH in human MDA-MB-468 cells assessed as decrease in serine flux, EC50 = 2.3 μM. 29555419
MDA-MB-468 Cytotoxicity assay Cytotoxicity against human MDA-MB-468 cells, EC50 = 8 μM. 29555419
Click to View More Cell Line Experimental Data

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 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]
Kinase Assay 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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Mcm2 / Mcm2 25412417
In Vivo
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]
Animal Research Animal Models Mice bearing Colo-205 xenografts
Dosages ~100 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00886782 Terminated
Advanced Solid Cancers|Metastatic Cancer
Bristol-Myers Squibb|Exelixis
 May 31 2009 Phase 1|Phase 2
NCT00838890 Terminated
Refractory Hematologic Cancer
Bristol-Myers Squibb|Exelixis
 March 2009 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 326.18 Formula

C14H13Cl2N3O2
CAS No. 1169562-71-3 SDF Download XL413 SDF
Smiles C1CC(NC1)C2=NC3=C(C(=O)N2)OC4=C3C=C(C=C4)Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 46 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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