ChemicalBook--->CAS DataBase List--->933786-58-4

933786-58-4

933786-58-4 Structure

933786-58-4 Structure
IdentificationBack Directory
[Name]

CAY10561
[CAS]

933786-58-4
[Synonyms]

CAY10561
CAY-10561,CAY10561
CAY10561 Exclusive
YMUYGRBBEDYUOP-UHFFFAOYSA-N
PYRAZOLYLPYRROLE ERK INHIBITOR
[Molecular Formula]

C22H17Cl2FN4O2
[MDL Number]

MFCD10567088
[MOL File]

933786-58-4.mol
[Molecular Weight]

459.3
Chemical PropertiesBack Directory
[Boiling point ]

733.2±60.0 °C(Predicted)
[density ]

1.463±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 2.5 mg/ml; DMSO: 1.5 mg/ml; Ethanol: 5 mg/ml; Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml
[form ]

A crystalline solid
[pka]

12.89±0.50(Predicted)
Hazard InformationBack Directory
[Description]

The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary.1 CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM).2 This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 μM) and JNK3 (Ki = 4 μM).2 CAY10561 inhibits proliferation of COLO 205 cells with an IC50 value of 0.54 μM.2
[Uses]

ERK2-IN-4 (Compound 6o) is an effective and selective ERK2 inhibitor with a Ki of 0.006 μM. ERK2-IN-4 inhibits the ERK signaling pathway and can be used in cancer research[1].
[IC 50]

ERK2: 0.006 μM (Ki)
[References]

1. Junttila, M.R., Li, S.P., and Westermarck, J. Phosphatase-mediated crosstalk between MAPK signaling pathways in the regulation of cell survival FASEB J. 22,1-12(2008).
2. Aronov, A.M., Baker, C., Bemis, G.W., et al. Flipped out: Structure-guided of selective pyrazolylpyrrole ERK inhibitors J. Med. Chem. 50,1280-1287(2007).
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