NPS-1034 is a novel MET inhibitor, which inhibits the activated MET receptor and its constitutively active mutants. NPS-1034, inhibits various constitutively active mutant forms of MET as well as HGF-activated wild-type MET. NPS-1034 inhibited the proliferation of cells expressing activated MET and promoted the regression of tumors formed from such cells in a mouse xenograft model through anti-angiogenic and pro-apoptotic actions. NPS-1034 also inhibited HGF-stimulated activation of MET signaling in the presence or absence of serum. Notably, NPS-1034 inhibited three MET variants that are resistant to the MET inhibitors SU11274, NVP-BVU972, and PHA665752.
MedKoo Cat#: 406461
Name: NPS-1034
CAS#: 1221713-92-3
Chemical Formula: C31H23F2N5O3
Exact Mass: 551.1769
Molecular Weight: 551.54
Elemental Analysis: C, 67.51; H, 4.20; F, 6.89; N, 12.70; O, 8.70
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 20.0 | 36.26 | |
| DMSO | 29.5 | 53.49 | |
| DMSO:PBS (pH 7.2) (1:5) | 0.2 | 0.29 | |
| Ethanol | 2.5 | 4.51 |
The following data is based on the product molecular weight 551.54 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 |
