Mefuparib HCl is a potent, highly selective, competitive PARP1/2 inhibitor with IC50 of 3.2/1.9 nM, respectively; displays >406-fold over other major nuclear PARPs including PARP3, TNKS1, TNKS2 and PARP6; reduces poly(ADP-ribose) formation, enhances γH2AX levels, induces G2/M arrest and subsequent apoptosis in homologous recombination repair (HR)-deficient cells; shows potent in vitro and in vivo proliferation and growth inhibition against HR-deficient cancer cells and synergistic sensitization of HR-proficient xenografts to the anticancer drug temozolomide.
MedKoo Cat#: 413393
Name: Mefuparib HCl
CAS#: 1449746-00-2 (HCl)
Chemical Formula: C17H16ClFN2O2
Exact Mass: 334.0884
Molecular Weight: 334.78
Elemental Analysis: C, 60.99; H, 4.82; Cl, 10.59; F, 5.67; N, 8.37; O, 9.56
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 334.78 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 |
