XL413 (BMS-863233)

Catalog No.S7547

For research use only.

XL413 (BMS-863233) 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. Phase 1/2.

XL413 (BMS-863233) Chemical Structure

CAS No. 1169562-71-3

Selleck's XL413 (BMS-863233) has been cited by 13 publications

Purity & Quality Control

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Biological Activity

Description XL413 (BMS-863233) 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. Phase 1/2.
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231T cells MoflSpVv[3Srb36gZZN{[Xl? Mo\jOEBp NGjHPHhKdmirYnn0bY9vKG:oIFPER|chcW5iaIXtZY4hVUSDLV3CMVI{OVRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBOS01{IIDoc5NxcG:{eXzheIlwdiCjdDDT[ZI2OyCjZoTldkA1KGi{czygTWM2OD1yLkGxPEDPxE1? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV4MEW2O{c,OjJ3NkC1Olc9N2F-
human Caco2 cells NGPERXVHfW6ldHnvckBie3OjeR?= M2Da[|QhcA>? NWTCW3Y6UW6qaXLpeIlwdiCxZjDDSGM4KGmwIHj1cYFvKEOjY3:yJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTVPNNkBxcG:|cHjvdplt[XSrb36gZZQhW2W{NUOgZYZ1\XJiNDDodpMtKEmFNUC9NE4yPCEQvF2= NXmydI41RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OlA2PjdpPkKyOVYxPTZ5PD;hQi=>
human Caco2 cells NFX4NodRem:uaX\ldoF1cW:wIHHzd4F6 NVjuOYpESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDZYNwOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIghcW5ic3;meEBi\2G{LDDJR|UxRTBwN{G1JO69VQ>? NHTFbVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW2NFU3Pyd-MkK1OlA2Pjd:L3G+
Caco2 cells NFvpXXpHfW6ldHnvckBie3OjeR?= M3HFemlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iQ3Hjc|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iY3HzdIF{\SB|L{egZYN1cX[rdImsJGVEPTB;Mj6yPFgh|ryP MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV4MEW2O{c,OjJ3NkC1Olc9N2F-
MDA-MB-468 MVzGeY5kfGmxbjDhd5NigQ>? MVXJcohq[mm2aX;uJI9nKFCKR1TIJIlvKGi3bXHuJG1FSS2PQj20Olgh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5ic3XybY5mKG[udYisJGVEPTBiPTCyMlMh|ryPLh?= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV3NUSxPUc,Ojl3NUW0NVk9N2F-
MDA-MB-468 MkDhR5l1d3SxeHnjbZR6KGG|c3H5 MkDhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUS2PEBk\WyuczygSWM2OCB;IEig{txONg>? NIrxXpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW1OVQyQSd-Mkm1OVU1OTl:L3G+
Assay
Methods Test Index PMID
Western blot p-Mcm2 / Mcm2 25412417
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 Research:

[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.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: Mice bearing Colo-205 xenografts
  • Dosages: ~100 mg/kg
  • Administration: p.o.
  • (Only for Reference)

Solubility (25°C)

In vitro

Water 46 mg/mL warmed
(141.02 mM)
DMSO Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 326.18
Formula

C14H13Cl2N3O2

CAS No. 1169562-71-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(NC1)C2=NC3=C(C(=O)N2)OC4=C3C=C(C=C4)Cl.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00886782 Terminated Drug: Cdc7-inhibitor Advanced Solid Cancers|Metastatic Cancer Bristol-Myers Squibb|Exelixis May 2009 Phase 1|Phase 2
NCT00838890 Terminated Drug: Cdc7-inhibitor (BMS-863233) Refractory Hematologic Cancer Bristol-Myers Squibb|Exelixis March 2009 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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