Name | NU7026 |
Synonyms | CS-595 NU7026 NU 7026 NU-7026 LY293646 LY 293646 2-MORPHOLINO-4H-BENZO[H]CHROMEN-4-ONE 2-(4-Morpholinyl)-4H-naphthol[1,2-b]pyran-4-one |
CAS | 154447-35-5 |
Molecular Formula | C17H15NO3 |
Molar Mass | 281.31 |
Density | 1.330 |
Melting Point | 267-269 °C(Solv: methanol (67-56-1); water (7732-18-5)) |
Boling Point | 459.9±45.0 °C(Predicted) |
Solubility | Soluble in DMSO (3 mg/ml) at 60 °C, methanol (700 μg/ml), DMF (~0.15 mg/ml), and DMSO |
Appearance | solid |
Color | tan |
pKa | 0.49±0.20(Predicted) |
Storage Condition | 2-8°C |
MDL | MFCD06798345 |
In vitro study | NU7026 dose-dependently enhances ionizing radiation-induced cytotoxicity in both V3YAC and PARP-1 +/+ cells. NU7026 completely abolished the recovery of potentially lethal injury in growth-arrested cells. NU7026 inhibited 56% of DNA DSB repair in the V3 YAC cell line. In K562 cells, NU7026 (10 μm) enhanced the growth inhibition of idarubicin,daunorubicin,doxorubicin,etoposide,mAMSA, and mitoxantrone, with PF50 values in the range of approximately 19 (vs. mAMSA). To 2 (to idarubicin). NU7026 (10 μm) also enhanced etoposide growth inhibition in leukemic cells with a PF50 value of 10.53. NU7026 (10 μm) enhanced etoposide-induced G2 phase arrest in K562 cells. NU7026 enhances the toxicity of topo II, including inhibition of non-homologous end joining and G2/M checkpoint blockade. In CH1 human ovarian cancer cells, NU7026 (10 μm) exposure for 4 hours in combination with 3 Gy radiation is necessary for significant radiosensitization. In the CLL cell line (I83) and primary CLL-lymphocytes, NU7026 (< 10 μm) had synergistic cytotoxic activity with chlorambucil at the nontoxic dose of nu7026. NU7026 (10 μm) increased chlorambucil-induced G(2)/M phase arrest in I83 cells. In I83 cells, NU7026 (10 μm) enhanced chlorambucil-induced gamma H2AX throughout the cell cycle. NU7026 (10 μm) increased chlorambucil-induced apoptosis in the I83 cell line. NU7026 (55 μm) resulted in significant induction of telomere fusion in MEFs with p53 deletion and less telomeric fusion in MEFs with p53 and Ligase IV double deletion. |
In vivo study | NU7026(20mg/kg, I. v.) has a rapid plasma clearance (0.108/hr) in mice, which is largely due to extensive metabolism. The bioavailability of NU7026 after intraperitoneal (I. p.) or oral administration at a dose of 20 mg/kg was 20 and 15%, respectively. |
WGK Germany | 3 |