基本信息

产品描述

WHI-P180是多种激酶的抑制剂，对RET和KDR的IC50值分别为4.5 nM和66 nM。

靶点（IC50 & Targe）

CDK2

EGFR

体内研究

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-1 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, inhibited IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis[2].

参考文献

[1] Rebecca Newton, et al. Eur J Med Chem. 2016, 112: 20-32.

[2] Newton R, et al. Eur J Med Chem. 2016, 112:20-32.

产品说明

一般描述

A potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (Cdk2; IC₅₀ = 1 µM) by blocking the ATP site.
A potent inhibitor of lgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (Cdk2; IC₅₀ = 1 µM) by blocking the ATP site.

包装

1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Target IC₅₀: 1 µM for Cdk2
Primary Target
Cdk2
Product does not compete with ATP.
Reversible: no
Cell permeable: no

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Shewchuk, L., et al. 2000. J. Med. Chem. 43, 133.
Chen, C.L., et al. 1999. Pharm. Res. 16, 117.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息