U0126/U-0126

U0126/U-0126

U0126/U-0126

编号ABP000921 化学名称U0126/U-0126 CAS109511-58-2 分子式C18H16N6S2 分子量380.49 纯度 >99%

化学名称 : U0126/U-0126

CAS : 109511-58-2

英文名称: U0126/U-0126

英文同义词: 1,4-Diamino-2,3-dicyano-1,4-bis(o-aminophenylmercapto)butadiene

同义词: 1,4-Diamino-2,3-dicyano-1,4-bis(o-aminophenylmercapto)butadiene

Solubility:DMSO

Storage:at -20℃ 2 years

Biologieal

PD0325901 is non-competitive with ATP and is exquisitely specific and highly potent against purified MEK, exhibiting a Kiapp of 1 nM against activated MEK1 and MEK2. PD0325901 is roughly 500-fold more potent than CI-1040 with respect to its cellular effects on phosphorylation of ERK1 and ERK2, exhibiting subnanomolar activity.
A single oral dose of PD0325901 (25 mg/kg) suppressed phosphorylation of ERK by >50% at 24 hours post-dosing.
Anticancer activity of PD 0325901 has been demonstrated for a broad spectrum of human tumor xenografts, significantly inhibiting the growth of 6 out of 7 human tumor models tested. [1]

Reference

[1] Judith S. Sebolt-Leopold et al. Proc Amer Assoc Cancer Res.2004,45

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