ERK-IN-3


Catalog No. Size PriceQuantity
M23672-C Contact sales@xcessbio.com for quotation $100Unavailable

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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