| CAS NO: | 1169562-71-3 |
| 规格: | ≥98% |
| 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 |
| Molecular Weight (MW) | 326.18 |
|---|---|
| Formula | C14H13Cl2N3O2 |
| 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 info | Chemical 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 |
| Synonyms | XL413; BMS863233; XL-413; BMS-863233; XL 413; BMS 863233. |
| 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 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. |
| Animal model | Colo-205 xenograft model |
| Formulation & Dosage | 3, 100 mg/kg |
| References | Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. |
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