PD-184352

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 ATP 非竞争性 MEK1/2 抑制剂，在基于细胞的测定中 IC50 为 17 nM，对 MEK1/2 的选择性比 MEK5 高 100 倍。

A potent, ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, displays 100-fold more selective for MEK1/2 than MEK5; reduces pMAPK levels in multiple tumor cells, prevents cell cycle progression and induces G1 block; suppresses growth of colon tumors in vivo.Colon Cancer Phase 2 Discontinued(In Vitro):CI-1040 directly inhibits MEK1 with an IC50 of 17 nM. It has also been shown to have little activity against a panel of related kinases with IC50 values more than 2.5 orders of magnitude higher. Treatment of whole cells with CI-1040 completely inhibits the mitogen-stimulated phosphorylation of ERK. CI-1040 at a concentration of 1 μM is found to inhibit phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively in MDA-MB-231 breast cancer cells. CI-1040 induces apoptosis and inhibits proliferation in U-937 cells in a dose and time-dependent manner. CI-1040 induces a significant increase in PUMA mRNA and protein levels.(In Vivo):The systemic administration of the MEK inhibitor CI-1040 reduces adenoma formation to a third and significantly restores lung structure. The proliferation rate of lung cells of mice treated with CL-1040 is decreased without any obvious effects on differentiation of pneumocytes.

CI-1040 directly inhibits MEK1 with an IC50 of 17 nM. It has also been shown to have little activity against a panel of related kinases with IC50 values more than 2.5 orders of magnitude higher. Treatment of whole cells with CI-1040 completely inhibits the mitogen-stimulated phosphorylation of ERK. CI-1040 at a concentration of 1 μM is found to inhibit phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively in MDA-MB-231 breast cancer cells. CI-1040 induces apoptosis and inhibits proliferation in U-937 cells in a dose and time-dependent manner. CI-1040 induces a significant increase in PUMA mRNA and protein levels.

The systemic administration of the MEK inhibitor CI-1040 reduces adenoma formation to a third and significantly restores lung structure. The proliferation rate of lung cells of mice treated with CL-1040 is decreased without any obvious effects on differentiation of pneumocytes.

CI-1040

MAPK/ERK Signaling

MEK

MEK1|MEK2

Cancer

Colon Cancer

212631-79-3

478.6595

C17H14ClF2IN2O2

>98% (HPLC)

DMSO: ≥ 150 mg/mL

O=C(NOCC1CC1)C2=CC=C(F)C(F)=C2NC3=CC=C(I)C=C3Cl

Benzamide, 2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-

(-20℃)

With Ice Pack

≥ 2 years