WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 202462
Description: RO4987655, also known as CH4987655, is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. MEK inhibitor RO4987655 binds to and inhibits MEK, which may result in the inhibition of MEK-dependent cell signaling and the inhibition of tumor cell proliferation. MEK, a dual specificity threonine/tyrosine kinase, is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers.
MedKoo Cat#: 202462
Chemical Formula: C20H19F3IN3O5
Exact Mass: 565.03215
Molecular Weight: 565.28
Elemental Analysis: C, 42.49; H, 3.39; F, 10.08; I, 22.45; N, 7.43; O, 14.15
RO4987655, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Synonym: RO4987655; RO-4987655; RO 4987655; CH4987655; CH-4987655; CH 4987655.
IUPAC/Chemical Name: 3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)-5-((3-oxo-1,2-oxazinan-2-yl)methyl)benzamide
InChi Key: FIMYFEGKMOCQKT-UHFFFAOYSA-N
InChi Code: InChI=1S/C20H19F3IN3O5/c21-14-9-12(24)3-4-15(14)25-19-13(20(30)26-31-7-5-28)8-11(17(22)18(19)23)10-27-16(29)2-1-6-32-27/h3-4,8-9,25,28H,1-2,5-7,10H2,(H,26,30)
SMILES Code: O=C(NOCCO)C1=CC(CN2OCCCC2=O)=C(F)C(F)=C1NC3=CC=C(I)C=C3F
The following data is based on the product molecular weight 565.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Kraeber-BodÃ©rÃ© F, Carlier T, Naegelen VM, Shochat E, Lumbroso J, Trampal C, Nagarajah J, Chua S, Hugonnet F, Stokkel M, Gleeson F, Tessier J. Differences in the biologic activity of 2 novel MEK inhibitors revealed by 18F-FDG PET: analysis of imaging data from 2 phase I trials. J Nucl Med. 2012 Dec;53(12):1836-46. doi: 10.2967/jnumed.112.109421. Epub 2012 Nov 9. PubMed PMID: 23143089.
2: Leijen S, Middleton MR, Tresca P, Kraeber-BodÃ©rÃ© F, Dieras V, Scheulen ME, Gupta A, Lopez-Valverde V, Xu ZX, Rueger R, Tessier JJ, Shochat E, Blotner S, Naegelen VM, Schellens JH, Eberhardt WE. Phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of the MEK inhibitor RO4987655 (CH4987655) in patients with advanced solid tumors. Clin Cancer Res. 2012 Sep 1;18(17):4794-805. Epub 2012 Jul 5. PubMed PMID: 22767668.
3: Lee L, Niu H, Rueger R, Igawa Y, Deutsch J, Ishii N, Mu S, Sakamoto Y, Busse-Reid R, Gimmi C, Goelzer P, De Schepper S, Yoshimura Y, Barrett J, Ishikawa Y, Weissgerber G, Peck R. The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of CH4987655 in healthy volunteers: target suppression using a biomarker. Clin Cancer Res. 2009 Dec 1;15(23):7368-74. doi: 10.1158/1078-0432.CCR-09-1696. Epub 2009 Nov 24. PubMed PMID: 19934286.