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2062200-97-7

中文名稱 XL413 HYDROCHLORIDE
英文名稱 XL413 (hydrochloride)
CAS 2062200-97-7
分子式 C14H13Cl2N3O2
分子量 326.18
MOL 文件 2062200-97-7.mol
2062200-97-7 結(jié)構(gòu)式 2062200-97-7 結(jié)構(gòu)式

基本信息

中文別名
化合物XL413 HYDROCHLORIDE
英文別名
XL-413 hydrochloride,XL413 hydrochloride

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO:0.2(Max Conc. mg/mL);0.613(Max Conc. mM)
PBS (pH:7.2):10.0(Max Conc. mg/mL);30.66(Max Conc. mM)
形態(tài)結(jié)晶固體
顏色White to off-white

常見問題列表

生物活性
XL413 hydrochloride 是一種有效的,選擇性的,ATP 競爭性的 Cdc7 抑制劑,IC50 值為 3.4 nM,同時對 CK2 和 PIM1 的 IC50 值分別為 215 和 42 nM,對 pMCM 的 EC50 值為 118 nM。
靶點

Cdc7

3.4 nM (IC 50 )

PIM1

42 nM (IC 50 )

CK2

215 nM (IC 50 )

體外研究

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.

體內(nèi)研究

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.

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