BDP5290 HCl

BDP5290 HCl is a MRCK inhibitor.

Product information

CAS Number: 1817698-21-7

Molecular Weight: 408.29

Formula: C17H19Cl2N7O

Synonym:

BDP00005290

Chemical Name: 4-Chloro-1-(4-piperidyl)-N-[5-(2-pyridyl)-1H-pyrazol-4-yl]pyrazole-3-carboxamide Hydrochloride

Smiles: Cl.O=C(NC1C=NNC=1C1=CC=CC=N1)C1=NN(C=C1Cl)C1CCNCC1

InChiKey: AROXEVUAHBCZOW-UHFFFAOYSA-N

InChi: InChI=1S/C17H18ClN7O.ClH/c18-12-10-25(11-4-7-19-8-5-11)24-15(12)17(26)22-14-9-21-23-16(14)13-3-1-2-6-20-13;/h1-3,6,9-11,19H,4-5,7-8H2,(H,21,23)(H,22,26);1H

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 Ki of BDP5290 for MRCKα is 10 nM, which is slightly more than the Ki of 4 nM for MRCKβ. 3 μM BDP5290 completely inhibits myosin II light chain (MLC) phosphorylation induced by MRCKβ, but not by ROCK1 or ROCK2. At higher concentrations, BDP5290 reduces MLC phosphorylation (pMLC) to undetectable levels. BDP5290 reduces MDA-MB-231 invasion at all tested concentrations starting from 0.1 μM, with virtually complete inhibition at 10 μM. After 24 hours in the presence of BDP5290 cell viability is slightly reduced with an EC50  >10 μM. Wound closure is inhibited by >60% at 1 μM BDP5290, a concentration that has no effect on cell viability.

References:

1. Unbekandt M, et al. A novel small-molecule MRCK inhibitor blocks cancer cell invasion. Cell Commun Signal. 2014 Oct 5;12:54.

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