XL413 (hydrochloride)

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

XL413 抑制 MDA-MB-231T 和 COLO 205 细胞的生长（IC50 分别 = 118 和 140 nM），并减少 COLO 205 小鼠异种移植模型中的肿瘤生长。

XL413 is a potent inhibitor of Cdc7 (IC50 = 3.4 nM). It is >60, >10, and >300-fold selective for Cdc7 over CK2, PIM1, and a panel of over 100 protein kinases, respectively. XL413 inhibits the growth of MDA-MB-231T and COLO 205 cells (IC50s = 118 and 140 nM, respectively). It inhibits Cdc7-specific phosphorylation of mini-chromosome maintenance protein (MCM2) and induces cell cycle accumulation in the S and G2 phases in MDA-MB-231T and COLO 205 cells that overexpress Cdc7. In vivo, XL413 inhibits MCM2 phosphorylation (ED50 = <3 mg/kg) and reduces tumor growth in a COLO 205 mouse xenograft model when administered orally at doses of 10, 30, and 100 mg/kg.

XL413 (BMS-863233) hydrochloride inhibits the cell proliferation (IC50=2685 nM), decreases cell viability (IC50=2142 nM) and elicits the caspase 3/7 activity (EC50=2288 nM) in Colo-205 cells. XL413 hydrochloride also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC50=715 nM). XL413 hydrochloride shows cytotoxic effects on tumors, with IC50 of 22.9 μM in HCC1954 cells and 1.1 μM in Colo-205 cells. XL413 hydrochloride induces apoptosis in the Colo-205 cells, but not in HCC1954 cells. XL413 is effective DDK inhibitors in vitro, with IC50 of 22.7 nM. XL413 hydrochloride is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells.

XL413 (BMS-863233; 100 mg/kg, p.o.) hydrochloride shows excellent plasma exposures in mice and possesses good PK properties. XL413 (10, 30, or 100 mg/kg, p.o.) hydrochloride is well tolerated at all the doses, with no significant body weight loss.

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2062200-97-7

326.2

C14H12ClN3O2 ? HCl

>98% (HPLC)

H2O : 10 mg/mL (30.66 mM; Need ultrasonic)；DMSO : 3.4 mg/mL (10.42 mM; Need ultrasonic and warming)

O=C1N=C([C@@H]2CCCN2)NC3=C1OC4=C3C=C(Cl)C=C4.Cl

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(-20℃)

With Ice Pack

≥ 2 years