An ERK1/2 inhibitor
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Ulixertinib (hydrochloride)

Item No. 18298

Technical Information
Formal Name
4-[5-chloro-2-[(1-methylethyl)amino]-4-pyridinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide, monohydrochloride
CAS Number
1956366-10-1
Synonyms
  • BVD-523
  • VRT-752271
Molecular Formula
C21H22Cl2N4O2 • HCl
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 1 mg/ml
λmax
213, 252, 326 nm
SMILES
CC(C)NC1=CC(C2=CNC(C(N[C@H](CO)C3=CC(Cl)=CC=C3)=O)=C2)=C(Cl)C=N1.Cl
InChi Code
InChI=1S/C21H22Cl2N4O2.ClH/c1-12(2)26-20-8-16(17(23)10-25-20)14-7-18(24-9-14)21(29)27-19(11-28)13-4-3-5-15(22)6-13;/h3-10,12,19,24,28H,11H2,1-2H3,(H,25,26)(H,27,29);1H/t19-;/m1./s1
InChi Key
DKGYQCPFBWFTHM-FSRHSHDFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Ulixertinib is a reversible ERK1/2 inhibitor that demonstrates an IC50 value of <0.3 nM for ERK2.1 In A375 melanoma cells with b-RafV600E mutation, it has been reported to reduce the levels of phosphorylated ERK2 and the downstream kinase RSK (IC50s = 4.1 and 0.14 μM, respectively).1 Ulixertinib has also been shown to inhibit A375 cell proliferation with an IC50 value of 180 nM.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ward, R.A., Colclough, N., Challinor, M., et alStructure-guided design of highly selective and potent covalent inhibitors of ERK1/2. J. Med. Chem. 58(11), 4790-4801 (2015).