XL413 HYDROCHLORIDE
XL413 HYDROCHLORIDE 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMSO:0.2(最大浓度 mg/mL);0.613(最大浓度 mM) PBS (pH:7.2):10.0(最大浓度 mg/mL);30.66(最大浓度 mM) |
| 形态 | 结晶固体 |
XL413 HYDROCHLORIDE 用途与合成方法
|
Cdc7 3.4 nM (IC 50 ) |
PIM1 42 nM (IC 50 ) |
CK2 215 nM (IC 50 ) |
XL413 inhibits the cell proliferation (IC 50 = 2685 nM), decreases cell viability (IC 50 = 2142 nM) and elicits the caspase 3/7 activity (EC 50 = 2288 nM) in Colo-205 cells. XL413 also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC 50 = 715 nM). XL413 shows cytotoxic effects on tumors, with IC 50 of 22.9 µM in HCC1954 cells and 1.1 µM in Colo-205 cells. XL413 induces apoptosis in the Colo-205 cells, but not in HCC1954 cells. XL413 is effective DDK inhibitors in vitro, with IC 50 of 22.7 nM. XL413 is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells.
XL413 (100 mg/kg, p.o.) shows excellent plasma exposures in mice and possesses good PK properties. XL413 (10, 30, or 100 mg/kg, p.o.) is well tolerated at all the doses, with no significant body weight loss.
