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CAS No.: 1357470-29-1

Narazaciclib Catalog No. CSN17748

Synonyms: ON123300

ON123300 is a potent and multi-targeted kinase inhibitor which inhibits CDK4, Ark5, PDGFRβ, FGFR1, RET, and Fyn with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM respectively.

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实验方案

技术信息

生物活性

描述The cyclin-dependent kinases (CDKs) have a central role in coordinating the eukaryotic cell division cycle, and also serve to integrate diverse growth-regulatory signals^[5]. ON123300 is an effective multi-target kinase inhibitor against CDK4 and ARK5, two kinases intimately associated with growth, survival and metastasis of human tumor cells with IC₅₀s of 3.9 nM, 5 nM, respectively. Z138C cells treated with ON123300 for 24 hours accumulated in the G₁ phase at lower concentrations (0.1–1.0 µM), at higher concentrations of this compound, a large proportion of the cells progressed through the S and G₂/M phases of the cell cycle and eventually accumulated in the sub-G₁ phase, suggesting an induction of apoptosis. Granta 519 and Z138C cells were treated with increasing concentrations of ON123300 for 24 hours. ON123300 repressed the phosphorylation of pRb and p130 in a dose-dependent manner suggesting that ON123300 inactivated the Rb (Retinoblastoma family of proteins) pathway due to the inhibition of CDK4 in the two MCL (mantle cell lymphoma) cell lines. Mice with tumor xenografts were randomly assigned into 2 treatment groups and treated daily with either water (vehicle) or ON123300 (100mg/kg) on a daily basis. Treatment with ON123300 significantly inhibited (p<0.05) tumor growth over a 2-week period, suggesting that this compound is a potent inhibitor of MCL proliferation in vivo^[6].

动物研究

剂量

Rat: 5 mg/kg, 10 mg/kg^[3] (i.v.); 25 mg/kg, 200 mg/kg^[3] (p.o.) Mice: 125 mg/kg^[4] (p.o.)

给药途径

i.v., p.o.

动物药代数据

Animal	Rats^[3]
Dose	10 mg/kg
Administration	i.v.
V	4.72 ± 0.99 L/kg (male) 2.85 ± 0.17 L/kg (female)
T_1/2	0.71 ± 0.10 h (male) 0.87 ± 0.12 h (female)
CL	75.90 ± 4.66 ml/min/kg (male) 38.44 ± 4.60 ml/min/kg (female)
AUC_0→∞	2200 ± 136 ng·h/ml (male) 4399 ± 542 ng·h/ml (female)

参考文献

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
- 2.3282 mL
- 11.6410 mL
- 23.2819 mL
- 5 mM
- 0.4656 mL
- 2.3282 mL
- 4.6564 mL
- 10 mM
- 0.2328 mL
- 1.1641 mL
- 2.3282 mL

技术信息

CAS号

1357470-29-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H27N7O

运输

蓝冰

分子量

429.52

别名

ON123300

溶解度

DMSO	12.0 mg/mL (27.9 mM)
Water	insoluble

动物实验配方

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