1. Protein Tyrosine Kinase/RTK
  2. Discoidin Domain Receptor
  3. DDR1-IN-2

DDR1-IN-2 

Cat. No.: HY-U00444 Purity: 98.62%
Handling Instructions

DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.

For research use only. We do not sell to patients.

DDR1-IN-2 Chemical Structure

DDR1-IN-2 Chemical Structure

CAS No. : 1429617-90-2

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 253 In-stock
Estimated Time of Arrival: December 31
5 mg USD 210 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
25 mg USD 740 In-stock
Estimated Time of Arrival: December 31
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Description

DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.

IC50 & Target

IC50: 13.1 nM (DDR1), 203 nM (DDR2), 414 nM (Bcr-Abl), 2500 nM (c-Kit)[1]

In Vitro

DDR1-IN-2 (compound 1) is a potent inhibitor of DDR1, with an IC50 of 13.1 nM, and less potently inhibits DDR2, with an IC50 of 203 nM. DDR1-IN-2 also shows inhibitory activities against Bcr-Abl and c-Kit, with IC50s of 414 and 2500 nM, respectively[1].

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

Molecular Weight

546.59

Formula

C₃₀H₂₉F₃N₆O

CAS No.

1429617-90-2

SMILES

O=C(NC1=CC(C(F)(F)F)=CC(CN2CCN(C)CC2)=C1)C3=CC=C(CC)C(C#CC4=CN5C(N=C4)=CC=N5)=C3

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 : 62.5 mg/mL (114.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8295 mL 9.1476 mL 18.2952 mL
5 mM 0.3659 mL 1.8295 mL 3.6590 mL
10 mM 0.1830 mL 0.9148 mL 1.8295 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: ≥ 2.08 mg/mL (3.81 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

The effects of compounds (including DDR1-IN-2) on the kinases DDR1 and DDR2 are assessed by using a LanthaScreen Eu kinase activity assay technology. Kinase reactions are performed in a 10 µL solution in low-volume 384-well plates. The kinase reaction buffer consists 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 are initiated by the addition of 100 nM ATP in the presence of serially diluted compounds (DDR1-IN-2). The reactions are allowed to proceed for 1 h 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 are acquired on a multilabel reader. Data analysis and curve fitting are performed using GraphPad Prism4 software[1].

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

References

Purity: 98.62%

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Keywords:

DDR1-IN-2Discoidin Domain ReceptorInhibitorinhibitorinhibit

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DDR1-IN-2
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HY-U00444
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