Select your Country or Region

  • TargetMol | Compound LibraryArgentinaArgentina
  • TargetMol | Compound LibraryAustraliaAustralia
  • TargetMol | Compound LibraryAustriaAustria
  • TargetMol | Compound LibraryBelgiumBelgium
  • TargetMol | Compound LibraryBrazilBrazil
  • TargetMol | Compound LibraryBulgariaBulgaria
  • TargetMol | Compound LibraryCroatiaCroatia
  • TargetMol | Compound LibraryCyprusCyprus
  • TargetMol | Compound LibraryCzechCzech
  • TargetMol | Compound LibraryDenmarkDenmark
  • TargetMol | Compound LibraryEgyptEgypt
  • TargetMol | Compound LibraryEstoniaEstonia
  • TargetMol | Compound LibraryFinlandFinland
  • TargetMol | Compound LibraryFranceFrance
  • TargetMol | Compound LibraryGermanyGermany
  • TargetMol | Compound LibraryGreeceGreece
  • TargetMol | Compound LibraryHong KongHong Kong
  • TargetMol | Compound LibraryHungaryHungary
  • TargetMol | Compound LibraryIcelandIceland
  • TargetMol | Compound LibraryIndiaIndia
  • TargetMol | Compound LibraryIrelandIreland
  • TargetMol | Compound LibraryIsraelIsrael
  • TargetMol | Compound LibraryItalyItaly
  • TargetMol | Compound LibraryKoreaKorea
  • TargetMol | Compound LibraryLatviaLatvia
  • TargetMol | Compound LibraryLebanonLebanon
  • TargetMol | Compound LibraryMalaysiaMalaysia
  • TargetMol | Compound LibraryMaltaMalta
  • TargetMol | Compound LibraryMoroccoMorocco
  • TargetMol | Compound LibraryNetherlandsNetherlands
  • TargetMol | Compound LibraryNew ZealandNew Zealand
  • TargetMol | Compound LibraryNorwayNorway
  • TargetMol | Compound LibraryPolandPoland
  • TargetMol | Compound LibraryPortugalPortugal
  • TargetMol | Compound LibraryRomaniaRomania
  • TargetMol | Compound LibrarySingaporeSingapore
  • TargetMol | Compound LibrarySlovakiaSlovakia
  • TargetMol | Compound LibrarySloveniaSlovenia
  • TargetMol | Compound LibrarySpainSpain
  • TargetMol | Compound LibrarySwedenSweden
  • TargetMol | Compound LibrarySwitzerlandSwitzerland
  • TargetMol | Compound LibraryTaiwan,ChinaTaiwan,China
  • TargetMol | Compound LibraryThailandThailand
  • TargetMol | Compound LibraryTurkeyTurkey
  • TargetMol | Compound LibraryUnited KingdomUnited Kingdom
  • TargetMol | Compound LibraryUnited StatesUnited States
  • TargetMol | Compound LibraryOther CountriesOther Countries
Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

DDR1-IN-2

DDR1-IN-2
Contact us for more batch information
Select Batch
Purity:100%
Resource Download

DDR1-IN-2

Catalog No. T5402Cas No. 1429617-90-2
DDR1-IN-2 (DDR1 inhibitor 7rh) (DDR1 inhibitor 7rh) is a potent, selective, ATP-competitive Discoidin domain receptor 1 (DDR1) inhibitor (IC50: 6.8 nM in cell-free kinase assays).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePrice/USDAvailabilityQuantity
1 mg$44In Stock
5 mg$97In Stock
10 mg$175In Stock
25 mg$365In Stock
50 mg$557In Stock
100 mg$815In Stock
500 mg$1,630In Stock
1 mL x 10 mM (in DMSO)$127In Stock
Bulk & Custom
Add to Cart
Questions
View More

Related Compound Libraries of "DDR1-IN-2"

Product Introduction

Bioactivity
Description
DDR1-IN-2 (DDR1 inhibitor 7rh) (DDR1 inhibitor 7rh) is a potent, selective, ATP-competitive Discoidin domain receptor 1 (DDR1) inhibitor (IC50: 6.8 nM in cell-free kinase assays).
In vitro
DDR1-IN-2 inhibited the enzymatic activity of DDR1, with IC50 values of 6.8 nM, but were significantly less potent in suppressing the kinase activities of DDR2, Bcr-Abl, and c-Kit. It bound with DDR1 with a Kd value of 0.6 nM, while it was significantly less potent to the other 455 kinases tested. It also potently inhibited the proliferation of cancer cells expressing high levels of DDR1 and strongly suppressed cancer cell invasion, adhesion, and tumorigenicity [1]. Pharmacologic inhibition of DDR1 with an ATP-competitive orally available small-molecule kinase inhibitor (DDR1-IN-2) abrogated collagen-induced DDR1 signaling in pancreatic tumor cells and consequently reduced colony formation and migration [2].
In vivo
DDR1-IN-2 possessed good PK profiles, with oral bioavailabilities of 67.4% [1]. The inhibition of DDR1 with DDR1-IN-2 showed striking efficacy in combination with chemotherapy in orthotopic xenografts and autochthonous pancreatic tumors where it significantly reduced DDR1 activation and downstream signaling, reduced primary tumor burden, and improved chemoresponse [2].
Kinase Assay
The functional assays of compounds on the kinase activities of c-kit and Abl were determined using the FRET-based Z'-Lyte assay system according to the manufacturer's instructions. Tyrosine 2 Peptide was used as Abl substrate and Ser/Thr 6 peptide was used as the substrate for c-kit. The reactions were carried out in 384-well plates in a 10 μl of reaction volume with an appropriate amount of kinases in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM EGTA, and 0.01% Brij-35. The reactions were incubated 1 hour at room temperature in the presence of 2 μM of substrate with 10 μM of ATP (for Abl1 assays) or 300 μM of ATP (kit assay) and in the presence of various concentrations of the compounds. The development reagent was then added for further 2 hours room temperature incubation followed by the addition of stop solution. Fluorescence signal ratio of 445 nm (Coumarin)/520 nm (fluorescin) was examined on EnVision Multilabel Reader. The effects of compounds on the kinases DDR1 and DDR2 were assessed by using a LanthaScreen Eu kinase activity assay technology. Kinase reactions are performed in a 10 μL volume in low-volume 384-well plates. The kinases in reaction buffer consist of 50 mM HEPES pH 7.5, 0.01% BRIJ-35, 10 mM MgCl2, and 1 mM EGTA, the concentration of Fluorescein-Poly GAT Substrate in the assay is 100 nM, Kinase reactions were initiated with the addition of 100 nM ATP in the presence of serials of dilutions of compounds. The reactions were allowed to proceed for 1 hour at room temperature before a 10 μL preparation of EDTA (20 mM) and Eu-labeled antibody (4 nM) in TR-FRET dilution buffer are added. The final concentration of antibody in the assay well is 2 nM, and the final concentration of EDTA is 10 mM. The plate is allowed to incubate at room temperature for one more hour before the TR-FRET emission ratios of 665 nm/340 nm were acquired on a PerkinElmer EnVision Multilabel Reader [1].
Cell Research
Adherent Cells were plated in 96-well culture plates with a cell density of 3000-4000 cells/well and treated with indicated compounds by adding 100μL medium containing compounds of various concentrations on the second day. After 72-hour's treatment, MTT was added to each well and incubated for additional 4-5 hours, and the absorbance was measured on a microplate reader at 570nm. Cell growth inhibition was evaluated as the ratio of the absorbance of the sample to that of the control. The results are representative of at least 4 independent experiments [1].
Animal Research
Compounds 7rh and 7rj were dissolved in mixed solvents (DMSO : EtOH:Cremophor EL : H2O = 2 : 4 : 4 : 90) as clear solution. The final concentrations were 2.5 mg/mL. Sprague Dawley (SD) rats (male, 4 animals per group) weighted 180~220g were injected intravenously or administrated orally at doses of 5 mg/kg (i.v.) or 25mg/kg (p.o.), respectively. After dose administration, 0.3 mL of the orbital blood was taken at 2.0 min, 10.0 min, 30.0 min, 1.0 h, 2.0 h, 3.0 h, 4.0 h, 6.0 h, 8.0 h, 12.0 h, 21.0 h, 24.0 h, 30.0 h, 36.0 h, 48.0 h, and 72.0 h. Samples were stored at -70℃ until shipment to the analytical laboratory and tested by HPLC/MS using propranolol as internal standard to measure the compound concentration in the blood [1].
AliasDDR1 inhibitor 7rh
Chemical Properties
Molecular Weight546.59
FormulaC30H29F3N6O
Cas No.1429617-90-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 12 mg/mL (21.95 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8295 mL9.1476 mL18.2952 mL91.4762 mL
5 mM0.3659 mL1.8295 mL3.6590 mL18.2952 mL
10 mM0.1830 mL0.9148 mL1.8295 mL9.1476 mL
20 mM0.0915 mL0.4574 mL0.9148 mL4.5738 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg,each TargetMol | Animal experiments animal weighs 20 g, and the dosage volume is 100 μL. A total of TargetMol | Animal experiments 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL.
Mother liquor preparation method: 2 mg of drug dissolved in 50 μLDMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μLDMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords