Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
| Molecular Weight | 625.45 |
| CAS Number | 1206801-37-7 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage | 2-8°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related c-Met Products |
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| BMS-817378
BMS-817378 is a potent and selective inhibitor of MET with IC50 of 1.7 nM. |
| Capmatinib dihydrochloride hydrate
Capmatinib dihydrochloride hydrate is a potent, orally active, selective, ATP-competitive c-Met kinase inhibitor (IC50=0.13 nM) that inhibits the phosphorylation of c-MET, as well as downstream effector proteins of the c-MET pathway, such as ERK1/2, AKT, FAK, In addition, Capmatinib dihydrochloride hydrate effectively inhibited the proliferation and migration of c-Met-dependent tumor cells, induced apoptosis, and demonstrated antitumor activity in a mouse model of tumor. Capmatinib dihydrochloride hydrate is mainly metabolized by CYP3A4 and aldehyde oxidase. |
| Caveolin-1 (82-101) amide (human, mouse, rat)
Caveolin-1 (82-101) amide (human, mouse, rat) (Caveolin-1 scaffolding domain peptide) is a peptide that reverses aging-associated deleterious changes in multiple organs. |
| Norleual
Norleual, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. |
| Fosgonimeton
Fosgonimeton is a potentially first-in-class Hepatocyte Growth Factor Receptor (HGF) agonist that enhances HGF/MET signaling pathway activity for Alzheimer's Disease (AD) research. |
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