[CAS NO. 1206799-15-6] Merestinib (LY2801653)
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PRODUCTS SPECIFICATIONS [1206799-15-6]
Catalog
SLK-S7014
Brand
Selleck
CAS
1206799-15-6
DESCRIPTION [1206799-15-6]
Overview
| MDL | MFCD23160048 |
|---|---|
| Molecular Weight | 552.53 |
| Molecular Formula | C30H22F2N6O3 |
| SMILES | O=C(C1=CC=C(C)N(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=CC5=C(N(C)N=C5)C=C4C6=CNN=C6)C(F)=C3 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8099 mL | 9.0493 mL | 18.0986 mL |
| 5 mM | 0.3620 mL | 1.8099 mL | 3.6197 mL |
| 10 mM | 0.1810 mL | 0.9049 mL | 1.8099 mL |
| 50 mM | 0.0362 mL | 0.1810 mL | 0.3620 mL |
Description
Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits , , , , , , and with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
Targets
In vitro
LY2801653 demonstrates in vitro effects on MET pathway-dependent cell scattering and cell proliferation. It demonstrates more potent anti-proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) than the cell lines without MET gene amplification (U-87MG, KATO-III). LY2801653 also maintains potency against 13 MET variants, each bearing a single-point mutation. It is found to have potent activity against several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2 and against the serine/threonine kinases MKNK1/2. The mean IC50 value of LY2801653 for inhibition of MET auto-phosphorylation in HGF-stimulated H460 cells is 35.2±6.9 nM and the IC50 for MET auto-phosphorylation in S114 cells is 59.2 nM.
References
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