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CAS No. 1169562-71-3
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.
Selleck's XL413 (BMS-863233) has been cited by 10 publications
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The protein levels of p-MCM2 and p-ERK in NOK, HN6 and Cal27 cells treated with 0, 10 and 20 μMXL413 were detected by western blotting.
J Mol Med, 2018, 96(6):513-525. XL413 (BMS-863233) purchased from Selleck.
Effects of XL413 plus pirfenidone on 10T1/2 cells morphology, proliferation and TGF-β1-induced α-SMA expression. Cells were exposed to control, XL413 (10 μM), pirfenidone (1 mg/ml) or XL413 plus pirfenidone. (G) Laser confocal scanning was used for visualization of α-SMA protein expression and cellular morphological changes.
Exp Cell Res, 2015, 339(2):289-99.. XL413 (BMS-863233) purchased from Selleck.
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Choose Selective CDK Inhibitors
|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.|
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. 
|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. |
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.
|In vitro||Water||46 mg/mL warmed (141.02 mM)|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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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|
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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