XL413 (BMS-863233)

Catalog No.S7547

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.

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XL413 (BMS-863233) Chemical Structure

XL413 (BMS-863233) Chemical Structure
Molecular Weight: 326.18

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Quality Control & MSDS

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Product Description

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] Pim1 [1] CK2 [1]
IC50 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]
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]
Features

Protocol(Only for 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 Assay: [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.

Animal Study: [1]

Animal Models Mice bearing Colo-205 xenografts
Formulation
Dosages ~100 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Koltun ES, et al. Bioorg Med Chem Lett. 2012, 22(11), 3727-3731.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00838890 Terminated Refractory Hematologic Cancer Bristol-Myers Squibb|Exelixis March 2009 Phase 1|Phase 2

Chemical Information

Download XL413 (BMS-863233) SDF
Molecular Weight (MW) 326.18
Formula

C14H13Cl2N3O2

CAS No. 1169562-71-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro Water 46 mg/mL warming (141.02 mM)
DMSO <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or 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 Name Benzofuro[3,​2-​d]​pyrimidin-​4(3H)​-​one, 8-​chloro-​2-​(2S)​-​2-​pyrrolidinyl-​, hydrochloride

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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