RO4987655
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    WARNING: This product is for research use only, not for human or veterinary use.

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.


Chemical Structure

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RO4987655
CAS# 874101-00-5

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

Size Price Shipping out time Quantity
200mg USD 2650 2 Weeks
500mg USD 3850 2 Weeks
1g USD 4650 2 Weeks
2g USD 6950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-26. Prices are subject to change without notice.

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

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).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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.



Additional Information