1. MAPK/ERK Pathway
  2. MEK

Refametinib (Synonyms: BAY 869766; BAY 86-97661; RDEA119)

Cat. No.: HY-14691 Purity: 98.46%
Handling Instructions

Refametinib (RDEA119, BAY 86-9766), is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity (IC50=19 nM MEK1; IC50=47 nM MEK2).

For research use only. We do not sell to patients.
Refametinib Chemical Structure

Refametinib Chemical Structure

CAS No. : 923032-37-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 121 In-stock
5 mg USD 96 In-stock
10 mg USD 144 In-stock
50 mg USD 372 In-stock
100 mg USD 624 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Refametinib:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


Refametinib (RDEA119, BAY 86-9766), is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity (IC50=19 nM MEK1; IC50=47 nM MEK2). IC50 Value: 19 nM (MEK1); 47 nM (MEK2) [1] Target: MEK1; MEK2 in vitro: RDEA119 potently inhibited MEK activity in enzyme inhibition assays in a non-ATP-competitive manner (MEK1 IC50 = 19 nmol/L, MEK2 IC50 = 47 nmol/L) determined through incorporation of radioactive phosphate from ATP into ERK as substrate. RDEA119 potently inhibited MEK activity as measured by phosphorylation of ERK1/2 across several human cancer cell lines of different tissue origins and BRAF mutational status with EC50 values ranging from 2.5 to 15.8 nmol/L [1]. BAY 86-9766 exhibited potent antiproliferative activity in HCC cell lines with half-maximal inhibitory concentration values ranging from 33 to 762 nM. BAY 86-9766 was strongly synergistic with sorafenib in suppressing tumor cell proliferation and inhibiting phosphorylation of the extracellular signal-regulated kinase (ERK) [2]. in vivo: RDEA119/BAY 869766 exhibits potent activity in xenograft models of melanoma, colon, and epidermal carcinoma. RDEA119/BAY 869766 exhibits complete suppression of ERK phosphorylation at fully efficacious doses in mice. RDEA119/BAY 869766 shows a tissue selectivity that reduces its potential for central nervous system-related side effects [1]. BAY 86-9766 prolonged survival in Hep3B xenografts, murine Hepa129 allografts, and MH3924A rat allografts. Additionally, tumor growth, ascites formation, and serum alpha-fetoprotein levels were reduced. Synergistic effects in combination with sorafenib were shown in Huh-7, Hep3B xenografts, and MH3924A allografts [2].

Clinical Trial
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.7472 mL 8.7361 mL 17.4721 mL
5 mM 0.3494 mL 1.7472 mL 3.4944 mL
10 mM 0.1747 mL 0.8736 mL 1.7472 mL
Please refer to the solubility information to select the appropriate solvent.
Molecular Weight







O=S(C1(C[[email protected]](O)CO)CC1)(NC(C(NC(C(F)=C2)=CC=C2I)=C3F)=C(OC)C=C3F)=O

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 31 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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