[CAS NO. 1449685-96-4] DDR1-IN-1

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PRODUCTS SPECIFICATIONS [1449685-96-4]

Catalog

SLK-S7498

Brand

Selleck

CAS

1449685-96-4

DESCRIPTION [1449685-96-4]

Overview

MDL	-
Molecular Weight	552.59
Molecular Formula	C30H31F3N4O3
SMILES	O=C(NC1=CC=C(C)C(OC2=CC3=C(NC(C3)=O)C=C2)=C1)C4=CC=C(CN5CCN(CC)CC5)C(C(F)(F)F)=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8097 mL	9.0483 mL	18.0966 mL
5 mM	0.3619 mL	1.8097 mL	3.6193 mL
10 mM	0.1810 mL	0.9048 mL	1.8097 mL
50 mM	0.0362 mL	0.1810 mL	0.3619 mL

Description

DDR1-IN-1 is a potent and selective receptor tyrosine kinase inhibitor with of 105 nM, about 3-fold selectivity over DDR2.

Targets

DDR1 ^[1] (Cell-free assay)	DDR2 ^[1] (Cell-free assay)
105 nM	413 nM

In vitro

In U2OS cells, DDR1-IN-1 inhibits basal DDR1 autophosphorylation with EC50 of 86 nM, and demonstrates stronger inhibition of DDR1 autophosphorylation in the absence of collagen stimulation. In a panel of different cancer cell lines that possess DDR1 gain-of-function mutations and/or overexpression, DDR1-IN-1, dose not inhibit proliferation below a concentration of 10 μM, while GSK2126458 potentiates the antiproliferative activity of DDR1-IN-1.

References

[1] Kim HG, et al. ACS Chem Biol. 2013, 8(10), 2145-2150.