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.
For research use only. We do not sell to patients.
- CAS No.: 1635405-90-1
- Formula: C20H16FN7
- Molecular Weight:373.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
c-Met 1.45 nM (IC50) |
Cellular Effect
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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
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CAS No. 1635405-90-1
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Molecular Weight 373.40
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Formula C20H16FN7
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SMILES
FC=1C=C2N=CC=CC2=CC1C(N3C=NC=4N=CC(=NC43)C=5C=NN(C5)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)