GNE-495 is a potent and selective MAP4K4 Inhibitor with efficacy in retinal angiogenesis. GNE-495 showed excellent potency and good PK and was used to demonstrate in vivo efficacy in a retinal angiogenesis model recapitulating effects that were observed in the inducible Map4k4 knockout mice. Mitogen-activated protein kinase kinase kinase kinase (MAP4K4, or HGK), and its homologues Misshapen and MIG-15 have been shown to regulate a multitude of biological processes, including embryonic development,metabolism, inflammation, neural regeneration, angiogenesis, and cancer.
MedKoo Cat#: 522457
Name: GNE-495
CAS#: 1449277-10-4
Chemical Formula: C22H20FN5O2
Exact Mass: 405.1601
Molecular Weight: 405.43
Elemental Analysis: C, 65.18; H, 4.97; F, 4.69; N, 17.27; O, 7.89
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.6 | 8.85 | |
| DMSO:PBS (pH 7.2) (1:7) | 0.1 | 0.31 | |
| DMF | 5.0 | 12.33 | |
| Water | 1.0 | 2.47 |
The following data is based on the product molecular weight 405.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
