1D-2
1D-2 is a c-Met protein kinase inhibitor, with a human-derived IC50 of 1.45 nM. 1D-2 inhibits the proliferation of cancer cells and exhibits metabolic stability in human and rat liver microsomes. 1D-2 can be used in related research on non-small cell lung cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1635405-90-1
- Formel: C20H16FN7
- Molecular Weight:373.40
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
c-Met 1.45 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1993 | IC50 |
31.3 nM
Compound: 1D
|
Cytotoxicity against human NCI-H1993 cells assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against human NCI-H1993 cells assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 27448775] |
In Vitro
1D-2 (72 h) potently inhibits the proliferation of human non-small cell lung cancer NCI-H1993 cells, with an IC50 value of 24.7 nM[1].
1D-2 (5-10 min preincubation, 30 min kinase reaction, 1 h detection incubation) potently inhibits the activity of purified c-Met kinase, with an IC50 of 1.45 nM[1].
1D-2 (1 μM; preincubated for 5 min, followed by incubation with NADPH for 5-30 min) exhibits favorable metabolic stability in human liver microsomes (CLint = 8 μl/min/mg protein) and rat liver microsomes (CLint = 49 μl/min/mg protein)[1].
1D-2 (10 μM; preincubated for 5 min, followed by incubation with NADPH for 5-30 min) directly inhibits CYP2C9 in human liver microsomes, and exhibits no time-dependent inhibitory effect on all tested cytochrome P450 isoforms[1].
1D-2 exhibits extremely high selectivity for c-Met, with IC50 values > 1000 nM against the other 17 tested human tyrosine kinases [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 1635405-90-1
-
Molecular Weight 373.40
-
Formel C20H16FN7
-
SMILES
FC=1C=C2N=CC=CC2=CC1C(N3C=NC=4N=CC(=NC43)C=5C=NN(C5)C)C
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)