MERESTINIB
LY2801653
CAS: 1206799-15-6
Molecular Formula: C30H22F2N6O3
MERESTINIB - Names and Identifiers
MERESTINIB - Physico-chemical Properties
| Molecular Formula | C30H22F2N6O3 |
| Molar Mass | 552.53 |
| Density | 1.42±0.1 g/cm3(Predicted) |
| Boling Point | 795.3±60.0 °C(Predicted) |
| pKa | 10.83±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | LY2801653 has an effect on MET signaling pathway-dependent cell scattering and cell proliferation in vitro. LY2801653 had a more potent anti-proliferative effect in cell lines that overexpressed MET(MET gene amplification) (MKN45, Hs746T and H1993) than in those that did not express MET. LY2801653 is active on 13 mutant MET (single point mutation) and also on several other tyrosine kinase receptors: MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2, also has an inhibitory effect on the serine/arithmetic kinase MKNK1/2. LY2801653 inhibited MET autophosphorylation with an IC50 of 35.2±6.9 nM in H460 cells under HGF-stimulation and with an IC50 of 59.2 nM in S114 cells. |
| In vivo study | LY2801653 has potent anti-tumor activity and vascular normalization effects in xenograft models that amplify MET(MKN45), MET autocrine (U-87MG and KP4), and over-express MET(H441). LY280165 was able to induce normalization of blood vessels in xenograft tumors, and in the animal model studied, LY2801653 had the shortest elimination half-life of 2.9 hours in mice and 14.3 hours in non-human primates. Currently, LY2801653 is being studied in clinical phase 1 as a test drug against advanced cancer. |
MERESTINIB - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.81 ml | 9.049 ml | 18.099 ml |
| 5 mM | 0.362 ml | 1.81 ml | 3.62 ml |
| 10 mM | 0.181 ml | 0.905 ml | 1.81 ml |
| 5 mM | 0.036 ml | 0.181 ml | 0.362 ml |
Last Update：2024-01-02 23:10:35
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CAS: 1206799-15-6
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