DDR Inhibitor |
| Katalog-Nr.GC33361 |
DDR-Inhibitor ist ein potenter Inhibitor des DiscoidindomÄnenrezeptors (DDR) mit einem IC50-Wert von 3,3 nM fÜr DDR2 und zeigt eine 53-prozentige Hemmung von DDR1 bei 1,5 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1644069-80-6
Sample solution is provided at 25 µL, 10mM.
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DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
DDR Inhibitor (Example 6) is a potent DDR inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM[1].
[1]. Gordon Saxty, et al. Imidazo-condensed bicycles as inhibitors of discoidin domain receptors (ddrs)
Kinase experiment: | Europium Kinase binding assay is used. Compounds (DDR Inhibitor, etc.) are incubated with 0.5 nM DDR1 or 0.25 nM DDR2 for 1 hour at room temperature in low volume black 384 well assay plates containing 5 nM or 10 nM Kinase Tracer 178 respectively and 2 nM Europium labelled anti-GST antibody in assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA and 0.01 % BRIJ35). The ratio of fluorescence emission 665 nm/615 nm after excitation at 340 nm is obtained. IC50 values are determined from dose-response plots using nonlinear least-squares analysis[1]. |
References: [1]. Gordon Saxty, et al. Imidazo-condensed bicycles as inhibitors of discoidin domain receptors (ddrs) | |
| Cas No. | 1644069-80-6 | SDF | |
| Canonical SMILES | O=C(C1=CN=C2C=CC=CN21)NC3=CC(CNC(NC4=CC=CC(F)=C4)=O)=CC=C3C | ||
| Formula | C23H20FN5O2 | M.Wt | 417.44 |
| Löslichkeit | DMSO : 65 mg/mL (155.71 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3956 mL | 11.9778 mL | 23.9555 mL |
| 5 mM | 479.1 μL | 2.3956 mL | 4.7911 mL |
| 10 mM | 239.6 μL | 1.1978 mL | 2.3956 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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