Description
ERK-IN-3 is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 can be used for the research of cancers driven by RAS mutations.
Product information
CAS Number: 2055597-12-9
Molecular Weight: 473.93
Formula: C22H25ClFN7O2
Chemical Name: N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-{5-methyl-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1H-imidazole-4-carboxamide
Smiles: CC1=CN=C(NC2CCOCC2)N=C1N1C=C(N=C1)C(=O)N[C@H](CN)C1=CC(F)=CC(Cl)=C1
InChiKey: PWHIUQBBGPGFFV-GOSISDBHSA-N
InChi: InChI=1S/C22H25ClFN7O2/c1-13-10-26-22(28-17-2-4-33-5-3-17)30-20(13)31-11-19(27-12-31)21(32)29-18(9-25)14-6-15(23)8-16(24)7-14/h6-8,10-12,17-18H,2-5,9,25H2,1H3,(H,29,32)(H,26,28,30)/t18-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (527.50 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ERK-IN-3 inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines. ERK-IN-3 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines.
In Vivo:
ERK-IN-3 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice and was well tolerated at efficacious doses.
Products are for research use only. Not for human use.
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