DDR-TRK-1
Based on 1 Customer Validation
DDR-TRK-1, a chemical probe, is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.
For research use only. We do not sell to patients.
- Purity : 98.90%
- CAS No.: 1934246-19-1
- Formula: C26H23F3N6O
- Molecular Weight:492.50
-
Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-114311
FGFR1/DDR2 inhibitor 1FGFR1/DDR2 Inhibitor -
HY-U00444
7rh -
HY-156552
DDR1/2 inhibitor-2DDR1/DDR2 Inhibitor -
HY-13979
DDR1-IN-1DDR1 Inhibitor -
HY-13979A
DDR1-IN-1 dihydrochloride -
HY-114169
WRG-28DDR2 Allosteric Inhibitor -
HY-135401
VU6015929DDR1/2 Inhibitor -
HY-112545
DDR2-IN-1DDR2 Inhibitor -
HY-133670
DDR1-IN-6DDR1 Inhibitor -
HY-133669
DDR1-IN-5DDR1 Inhibitor -
HY-15514
Merestinibc-Met Inhibitor -
HY-W018931
DDR Inhibitor
Biological Activity
Description
IC50 & Target
IC50: 9.4 nM (DDR1)[1].
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
188 nM
Compound: 6j
|
Inhibition of human recombinant GST-tagged DDR2 expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by lance ultra kinase assay
Inhibition of human recombinant GST-tagged DDR2 expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by lance ultra kinase assay
|
[PMID: 27219676] |
| Sf9 | IC50 |
9.4 nM
Compound: 6j
|
Inhibition of human recombinant GST-tagged DDR1 (440 to 876 residues) expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by TR-FRET LanthaScreen assay
Inhibition of human recombinant GST-tagged DDR1 (440 to 876 residues) expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by TR-FRET LanthaScreen assay
|
[PMID: 27219676] |
| Sf9 | IC50 |
>10000 nM
Compound: 6j
|
Inhibition of human full length recombinant His-tagged ABL1 expressed in baculovirus infected Sf9 insect cells using tyrosine 2 peptide as substrate preincubated for 1 hr measured after 2 hrs in presence of ATP by FRET-based Z'-Lyte assay
Inhibition of human full length recombinant His-tagged ABL1 expressed in baculovirus infected Sf9 insect cells using tyrosine 2 peptide as substrate preincubated for 1 hr measured after 2 hrs in presence of ATP by FRET-based Z'-Lyte assay
|
[PMID: 27219676] |
In Vitro
DDR-TRK-1 is a promising candidate, with an IC50 value of 9.4 nM against DDR1. DDR-TRK-1 also exhibits reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T1/2 value of 1.25 h at an oral dose of 20 mg/kg in rats. However, the area under concentration time curve (AUC) value of DDR-TRK-1 in mice is obviously higher than that in rats, suggesting its good absorption property in mice. The DDR1 inhibition of DDR1-IN-3 is further validated by determining its binding affinity with the DDR1 protein. It is shown that DDR-TRK-1 bounds tightly to DDR1, with a binding constant (Kd) value of 4.7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1934246-19-1
-
Appearance Solid
-
Molecular Weight 492.50
-
Formula C26H23F3N6O
-
Color White to off-white
-
SMILES
O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C(C=C3)=CC4=C3[C@@H](C)CN(C4)C5=CN=CN=C5
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : 40 mg/mL (81.22 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
-
Data Sheet (274 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0305 mL | 10.1523 mL | 20.3046 mL | 50.7614 mL |
| 5 mM | 0.4061 mL | 2.0305 mL | 4.0609 mL | 10.1523 mL | |
| 10 mM | 0.2030 mL | 1.0152 mL | 2.0305 mL | 5.0761 mL | |
| 15 mM | 0.1354 mL | 0.6768 mL | 1.3536 mL | 3.3841 mL | |
| 20 mM | 0.1015 mL | 0.5076 mL | 1.0152 mL | 2.5381 mL | |
| 25 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0305 mL | |
| 30 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6920 mL | |
| 40 mM | 0.0508 mL | 0.2538 mL | 0.5076 mL | 1.2690 mL | |
| 50 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 60 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8460 mL | |
| 80 mM | 0.0254 mL | 0.1269 mL | 0.2538 mL | 0.6345 mL |
DDR-TRK-1 Related Classifications
HY-100695 Related Classifications
Powered by Bioz