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.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
c-Met 1.45 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1993 | IC50 |
31.3 nM
Compound: 1D
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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
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[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. Further protocols information, click here.
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.
Protocols
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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.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
1D-2 Related Classifications
HY-114572 Related Classifications
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