WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406198
CAS#: 947182-25-4
Description: RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf/MEK/ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation.
MedKoo Cat#: 406198
Name: RO5068760
CAS#: 947182-25-4
Chemical Formula: C28H27FIN3O6
Exact Mass: 647.09286
Molecular Weight: 647.43
Elemental Analysis: C, 51.94; H, 4.20; F, 2.93; I, 19.60; N, 6.49; O, 14.83
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Synonym: RO5068760; RO 5068760; RO-5068760.
IUPAC/Chemical Name: (2S,3S)-2-((R)-4-(4-((R)-2,3-dihydroxypropoxy)phenyl)-2,5-dioxoimidazolidin-1-yl)-N-(2-fluoro-4-iodophenyl)-3-phenylbutanamide
InChi Key: MEPDJWRMAAUPBM-VGUPLNMOSA-N
InChi Code: InChI=1S/C28H27FIN3O6/c1-16(17-5-3-2-4-6-17)25(26(36)31-23-12-9-19(30)13-22(23)29)33-27(37)24(32-28(33)38)18-7-10-21(11-8-18)39-15-20(35)14-34/h2-13,16,20,24-25,34-35H,14-15H2,1H3,(H,31,36)(H,32,38)/t16-,20+,24+,25-/m0/s1
SMILES Code: O=C(N1[C@@H](C(NC2=CC=C(C=C2F)I)=O)[C@@H](C)C3=CC=CC=C3)[C@@H](C4=CC=C(OC[C@H](O)CO)C=C4)NC1=O
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
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
The following data is based on the product molecular weight 647.43 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: Su F, Bradley WD, Wang Q, Yang H, Xu L, Higgins B, Kolinsky K, Packman K, Kim MJ, Trunzer K, Lee RJ, Schostack K, Carter J, Albert T, Germer S, Rosinski J, Martin M, Simcox ME, Lestini B, Heimbrook D, Bollag G. Resistance to selective BRAF inhibition can be mediated by modest upstream pathway activation. Cancer Res. 2012 Feb 15;72(4):969-78. doi: 10.1158/0008-5472.CAN-11-1875. Epub 2011 Dec 28. PubMed PMID: 22205714.
2: Lee L, Niu H, Goelzer P, Rueger R, Deutsch J, Busse-Reid R, DeSchepper S, Blotner S, Barrett J, Weissgerber G, Peck R. The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of RO5068760, an MEK inhibitor, in healthy volunteers: assessment of target suppression. J Clin Pharmacol. 2010 Dec;50(12):1397-405. doi: 10.1177/0091270010361254. Epub 2010 Apr 12. PubMed PMID: 20386016.
3: Daouti S, Higgins B, Kolinsky K, Packman K, Wang H, Rizzo C, Moliterni J, Huby N, Fotouhi N, Liu M, Goelzer P, Sandhu HK, Li JK, Railkar A, Heimbrook D, Niu H. Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models. Mol Cancer Ther. 2010 Jan;9(1):134-44. doi: 10.1158/1535-7163.MCT-09-0601. Epub 2010 Jan 6. PubMed PMID: 20053779.
