RO4987655
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MedKoo CAT#: 202462

CAS#: 874101-00-5

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.


Price and Availability

Size
Price

200mg
USD 2650
2g
USD 6950
Size
Price

500mg
USD 3850
5g
Ask price
Size
Price

1g
USD 4650

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. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 202462
Name: RO4987655
CAS#: 874101-00-5
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


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


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not soluble in water.

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
  
 
 
 
 


References

1: Kraeber-Bodéré 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-Bodéré 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.