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

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PRODUCTS SPECIFICATIONS [1449685-96-4]

Catalog

HY-13979

Brand

MCE

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. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC ₅₀ of 105 nM; 4-fold less potent for DDR2 (IC ₅₀ = 413 nM) ^[1] .

IC50 & Target

IC50: 105 nM (DDR1) ^[1] .

In Vitro

DDR1-IN-1 effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC ₅₀ = 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 (IC ₅₀ < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 180.97 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent 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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (4.52 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

* All of the co-solvents are available by MCE.

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.