WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406298
CAS#: 876755-27-0
Description: RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a broad spectrum of tumor models. RO4927350 inhibits not only ERK1/2 but also MEK1/2 phosphorylation. In cancer cells, high basal levels of phospho-MEK1/2 rather than phospho-ERK1/2 seem to correlate with greater sensitivity to RO4927350. Furthermore, RO4927350 prevents a feedback increase in MEK phosphorylation, which has been observed with other MEK inhibitors. RO4927350 represents a novel therapeutic modality in cancers with aberrant MAPK pathway activation.
MedKoo Cat#: 406298
Name: RO4927350
CAS#: 876755-27-0
Chemical Formula: C27H28N4O6S
Exact Mass: 536.17296
Molecular Weight: 536.6
Elemental Analysis: C, 60.43; H, 5.26; N, 10.44; O, 17.89; S, 5.98
This product is not in stock, which may be available by custom synthesis.
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Synonym: RO4927350; RO 4927350; RO-4927350.
IUPAC/Chemical Name: (2S,3S)-2-((R)-4-(4-(2-hydroxyethoxy)phenyl)-2,5-dioxoimidazolidin-1-yl)-3-phenyl-N-(4-propionylthiazol-2-yl)butanamide.
InChi Key: RKKBPPTYPGTSEA-FNVCAUGXSA-N
InChi Code: InChI=1S/C27H28N4O6S/c1-3-21(33)20-15-38-26(28-20)30-24(34)23(16(2)17-7-5-4-6-8-17)31-25(35)22(29-27(31)36)18-9-11-19(12-10-18)37-14-13-32/h4-12,15-16,22-23,32H,3,13-14H2,1-2H3,(H,29,36)(H,28,30,34)/t16-,22+,23-/m0/s1
SMILES Code: C[C@@H](C1=CC=CC=C1)[C@H](N(C(N[C@@H]2C3=CC=C(OCCO)C=C3)=O)C2=O)C(NC4=NC(C(CC)=O)=CS4)=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: >2 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 536.6 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: Daouti S, Wang H, Li WH, Higgins B, Kolinsky K, Packman K, Specian A Jr, Kong N, Huby N, Wen Y, Xiang Q, Podlaski FJ, He Y, Fotouhi N, Heimbrook D, Niu H. Characterization of a novel mitogen-activated protein kinase kinase 1/2 inhibitor with a unique mechanism of action for cancer therapy. Cancer Res. 2009 Mar 1;69(5):1924-32. doi: 10.1158/0008-5472.CAN-08-2627. Epub 2009 Feb 24. PubMed PMID: 19244124.
