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XL413(BMS-863233)HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
XL413(BMS-863233)HCl图片
CAS NO:1169562-71-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)326.18
FormulaC14H13Cl2N3O2
CAS No.1169562-71-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: <1 mg/mL
Water: 46 mg/mL (141.02 mM)
Ethanol: <1 mg/mL
Other infoChemical Name: (S)-8-chloro-2-(pyrrolidin-2-yl)benzofuro[3,2-d]pyrimidin-4(3H)-one hydrochloride

InChi Key: UNDKJUKLBNARIZ-FVGYRXGTSA-N

InChi Code: InChI=1S/C14H12ClN3O2.ClH/c15-7-3-4-10-8(6-7)11-12(20-10)14(19)18-13(17-11)9-2-1-5-16-9;/h3-4,6,9,16H,1-2,5H2,(H,17,18,19);1H/t9-;/m0./s1

SMILES Code: O=C1C(OC2=CC=C(Cl)C=C23)=C3N=C([C@H]4NCCC4)N1.[H]Cl

SynonymsXL413; BMS863233; XL-413; BMS-863233; XL 413; BMS 863233.
实验参考方法
In Vitro

In vitro activity: 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.


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: The cell proliferation is measured by BrdU incorporation assay, and viability is assayed by Cell Titer–Glo kits. Celllin used: Colo-205 cells.

In VivoIn 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.
Animal modelColo-205 xenograft model
Formulation & Dosage3, 100 mg/kg
References

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31.