DDR1-IN-1 dihydrochloride


Catalog No. Size PriceQuantity
M13287-2 Contact sales@xcessbio.com for quotation $100
M13287-10 Contact sales@xcessbio.com for quotation $100

Description

DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM).

Product information

CAS Number: 1780303-76-5

Molecular Weight: 625.51

Formula: C30H33Cl2F3N4O3

Chemical Name: 4-[(4-ethylpiperazin-1-yl)methyl]-N-{4-methyl-3-[(2-oxo-2,3-dihydro-1H-indol-5-yl)oxy]phenyl}-3-(trifluoromethyl)benzamide dihydrochloride

Smiles: Cl.Cl.CC1C=CC(=CC=1OC1=CC2CC(=O)NC=2C=C1)NC(=O)C1C=C(C(CN2CCN(CC2)CC)=CC=1)C(F)(F)F

InChiKey: PBUOJKYQZINPKD-UHFFFAOYSA-N

InChi: InChI=1S/C30H31F3N4O3.2ClH/c1-3-36-10-12-37(13-11-36)18-21-6-5-20(15-25(21)30(31,32)33)29(39)34-23-7-4-19(2)27(17-23)40-24-8-9-26-22(14-24)16-28(38)35-26;;/h4-9,14-15,17H,3,10-13,16,18H2,1-2H3,(H,34,39)(H,35,38);2*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:

DDR1-IN-1 effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture.

References:

  1. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50.

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

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