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Home > Inhibitors & Agonists > Ras-Raf-MAPK-ERK > MEK (MAP2K)

RO4987655

  Cat. No.:  DC7488   Featured
Chemical Structure
874101-00-5
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More than 5000 active chemicals with high quality for research!
Field of application
RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 874101-00-5
Chemical Name: RO-4987655; RO 4987655; CH-4987655; CH4987655; CH 4987655
Synonyms: RO-4987655; RO 4987655; CH-4987655; CH4987655; CH 4987655
SMILES: FC(C(F)=C(NC1=CC=C(I)C=C1F)C(C(NOCCO)=O)=C2)=C2CN3C(CCCO3)=O
Formula: C20H19F3In3O5
M.Wt: 565.28
Description: RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
In Vivo: Single-agent oral administration of RO4987655 (CH4987655) results in complete tumor regressions in xenograft models. RO4987655 is rapidly absorbed with a tmax of ~1 h. Exposures are dose proportional from 0.5 to 4 mg. The disposition is biphasic with a terminal t1/2 of ~25 hr. Intersubject variability is low, 9% to 23% for Cmax and 14% to 25% for area-under-the-curve (AUC). pERK inhibition is exposure dependent and is greater than 80% inhibition at higher doses. The pharmacokinetic-pharmacodynamic relationship is characterized by an inhibitory Emax model (Emax ~100%; IC50 40.6 ng/mL) using nonlinear mixed-effect modeling[1]. Female athymic nude mice are randomized into study groups. The tumors size is estimated with digital caliper and PET scans performed on days 0, 1, and 3 with 1.0, 2.5, and 5.0 mg/kg RO4987655. The vehicle treatment does not inhibit the NCI-H2122 tumor xenograft growth over this time frame. In contrast, RO4987655 treatment results in 119% tumor growth inhibition (TGI) at 1.0 mg/kg, 145% TGI at 2.5 mg/kg and 150% TGI at 5.0 mg/kg on day 3. PET imaging shows that [18F] FDG uptake in the xenografts decreases within 24 h (day 1) from the administration of RO4987655[2].
In Vitro: RO4987655 potently inhibits mitogen-activated protein kinase signaling pathway activation and tumor cell growth, with an in vitro IC50 of 5.2 nM for inhibition of MEK1/2[1]. RO4987655 inhibits proliferation of NCI-H2122 cells in a dose-dependent manner with an IC50 value of 0.0065 μM. RO4987655 at doses ranging from 0.1 to 1.0 μM suppresses pERK1/2 already at 2 h after the start of treatment[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7488 RO4987655 RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.
DC7308 TAK-733 TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.
DC8401 BI-847325 BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
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