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CAS No.: 211555-08-7

WHI-P180/WHI-P180，盐酸盐 Catalog No. CSN16984

Synonyms: Janex 3

WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 μM, respectively.

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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 CDK2

IC50:1.0μM EGFR

IC50:4μM
描述The RET receptor tyrosine kinase is crucial for normal development but also contributes to pathologies that reflect both the loss and the gain of RET function^[3]. WHI-P180 is a multi-kinase inhibitor which inhibits RET, KDR and epidermal growth factor receptor (EGFR) with IC₅₀s of 5 nM, 66 nM and 4 μM, respectively^[4]. WHI-P180 is also an active inhibitor of IgE-mediated mast cell responses. The elimination half-life of WHI-P180 in CD-1 mice (BALB/c mice) following i.v., i.p., or p.o. administration is less than 10 min. Systemic clearance of WHI-P180 is 6742 mL/h/kg in CD-I mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive nontoxic i.p. bolus doses of 25 mg/kg, inhibits IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis^[5].

动物研究

剂量

CD-1 mice^[2]: 20 mg/kg (i.v. or i.p.); 200 mg/kg (p.o.) BALB/c mice^[2]: 20 mg/kg (i.v. or i.p.)

给药途径

i.v., i.p., p.o.

动物药代数据

Animal	Mice^[2]
Dose	20 mg/kg (i.v. or i.p., CD-1 mice) 200 mg/kg (p.o., CD-1 mice)
Administration	i.v. i.p. p.o.
F	26.7% (i.p.) 8.3% (p.o.)
V_c	634 ± 149 ml/kg (i.v.) 648 ± 59 ml/kg (i.p.) 450 ± 63 ml/kg (p.o.)
T_1/2	3.9 ± 0.5 h (i.v.) 4.0 ± 0.2 h (i.p.) 2.8 ± 6.7 h (p.o.)
T_max	0.7 ± 0.1 h (i.p.) 4.0 ± 0.5 h (p.o.)
C_max	110.4 ± 16.8 μM (i.v.) 25.7 ± 2.6 μM (i.p.) 48.0 ± 6.9 μM (p.o.)
CL_s	6742 ± 665 ml/kg (i.v.) 25214 ± 1536 ml/kg (i.p.) 81591 ± 17033 ml/kg (p.o.)
T_1/2α	0.1 ± 0.1 h (i.p.) 2.7 ± 0.2 h (p.o.)
AUC	10.4 ± 1.3 μM·h (i.v.) 2.8 ± 0.2 μM·h (i.p.) 8.6 ± 1.4 μM·h (p.o.)

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
- 3.3635 mL
- 16.8175 mL
- 33.6351 mL
- 5 mM
- 0.6727 mL
- 3.3635 mL
- 6.7270 mL
- 10 mM
- 0.3364 mL
- 1.6818 mL
- 3.3635 mL

技术信息

CAS号

211555-08-7

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H15N3O3

运输

蓝冰

分子量

297.31

别名

Janex 3

溶解度

DMSO	59.0 mg/mL (198.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
CDK2		IC50:1.0μM
EGFR		IC50:4μM

WHI-P180/WHI-P180，盐酸盐 Catalog No. CSN16984

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