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CAS No.: 1169562-71-3

XL 413 盐酸盐 Catalog No. CSN16423

Synonyms: BMS-863233 HCl;BMS-863233

XL413 HCl is a potent and selective Cdc7 inhibitor with an IC50 of 3.7 nM, > 60-fold selectivity against CK2, > 10-fold selectivity against PIM, and > 300-fold selectivity against a panel of over 100 protein kinases.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Casein Kinase 2

IC50:212nM Pim1

IC50:42nM CDC7

IC50:3.4nM
描述Cell division cycle 7 homolog (CDC7) is a serine/threonine kinase that plays a critical role in the initiation of DNA synthesis and in S phase cell cycle check point control. CDC7's role in DNA unwinding is essential for DNA replication, and subsequent cell proliferation. XL413 is a highly potent and selective CDC7 kinase inhibitor with IC₅₀ of 3.4 nM. Flow cytometry analysis of Colo-205 cells treated for 24 h with 1.1, 3.3, or 10 μM of XL413 causes dose-dependent accumulation of cells in the late S and G2 phases of the cell cycle, consistent with impaired DNA synthesis. Prolonged treatment with XL413 (3 days) inhibited the cell proliferation (IC₅₀ = 2685 nM), decreased cell via-bility (IC₅₀ = 2142 nM) and elicited the caspase 3/7 activity (EC₅₀ = 2288 nM) in Colo-205 cells. In addition, XL413 also significantly inhibited the anchorage-independent growth of colo-205 in soft agar (IC₅₀ = 715 nM). Those data indicated inhibition CDC7 with XL413 results in modified S phase progression that subsequently leads to apoptotic cell death. In a Colo-205 xenograft model, dose dependent target modulation was observed and a 70% inhibition of phosphorylated MCM2 (mini-chromosome maintenance protein) was detected even at the 3 mg/kg dose of XL413. The ED₅₀ was calculated to be <3 mg/kg. Tumor bearing mice were administered XL413 orally at doses of 30 mg/kg once daily (qd) for 14 days. Significant tumor growth inhibition (83%) was observed. More impressively, significant tumor growth regression (32%) was observed if dosed twice-daily at 30 mg/kg. The ED₅₀ is estimated at 13 mg/kg.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
Caco2 cells	-	Function assay	-	Induction of apoptosis in human Caco2 cells assessed as increase in caspase 3/7 activity, EC50=2.288 μM	22560567
human Caco2 cells	-	Function assay	4 h	Inhibition of CDC7 in human Caco2 cells assessed as inhibition of MCM2 phosphorylation at Ser53 after 4 hrs, IC50=0.14 μM	22560567
human Caco2 cells	-	Proliferation assay	-	Antiproliferative activity against human Caco2 cells assessed as inhibition of anchorage-independent growth in soft agar, IC50=0.715 μM	22560567

动物研究

剂量

Mice: 3 mg/kg- 100 mg/kg^[1] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Rats^[1]
Dose	3 mg/kg
Administration	i.v. p.o.
F	0.95
T_1/2	2.32 h
AUC	75 μM·h (p.o.)
CL	117 ml/h kg
C_max	8.61 μM (p.o.)
Vss	0.55 L/kg

参考文献

[1] Koltun ES, Tsuhako AL, et al. Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0658 mL
- 15.3291 mL
- 30.6581 mL
- 5 mM
- 0.6132 mL
- 3.0658 mL
- 6.1316 mL
- 10 mM
- 0.3066 mL
- 1.5329 mL
- 3.0658 mL

技术信息

CAS号

1169562-71-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H13Cl2N3O2

运输

蓝冰

分子量

326.18

别名

BMS-863233 HCl;BMS-863233

溶解度

DMSO	25.0 mg/mL (76.6 mM)

动物实验配方

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靶点	Description	IC50
Casein Kinase 2		IC50:212nM
Pim1		IC50:42nM
CDC7		IC50:3.4nM

XL 413 盐酸盐 Catalog No. CSN16423

靶点选择性

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