ERK-IN-2

ERK-IN-2 is a ERK2 inhibitor probe with an IC50 value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM.

Product information

Molecular Weight: 347.80

Formula: C16H18ClN5O2

Chemical Name: 3-[4-(hydroxymethyl)-1H-pyrazolo[4,3-c]pyridin-6-yl]-1-[(1R)-1-phenylethyl]urea hydrochloride

Smiles: Cl.C[C@@H](NC(=O)NC1=CC2NN=CC=2C(CO)=N1)C1C=CC=CC=1

InChiKey: VPFDSSKZNLUCLT-HNCPQSOCSA-N

InChi: InChI=1S/C16H17N5O2.ClH/c1-10(11-5-3-2-4-6-11)18-16(23)20-15-7-13-12(8-17-21-13)14(9-22)19-15;/h2-8,10,22H,9H2,1H3,(H,17,21)(H2,18,19,20,23);1H/t10-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

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:

The criteria of inhibitor probe: Inhibitor potency: goal is <100 nM (IC50); Selectively with target family: >30-fold. We recommend ERK-IN-2 (MRK-ERKi) to be used at a concentration of 1 μM in cell-based experiments and do not recommend doses >10 μM to be employed in any experiment. ERK-IN-2 (1 μM) has effects on cell proliferation in cancer cell lines. The IC50 values are 214 nM; 305 nM; 91 nM and 201 nM for A375SM cell, SK-MEL 30 cell; Colo 205 cell and Lovo cell, respectively.

In Vivo:

ERK-IN-2 (1 mpk; orally administation/0.5 mpk; intravenous injection) shows a DMPK value: h/r/d LM CLint: <17/235/<75 (mL/min/kg); uCLp:217 mL/min/kg; uVd 5.7 L/kg; t1/2: 0.4 h; rat F:13% in SD rat.

References:

1. MRK-ERK Inhibitor and Negative Control

Products are for research use only. Not for human use.