Molecular Formula | C23H29ClN4O2S |
Molar Mass | 461.02 |
Density | 1.30±0.1 g/cm3(Predicted) |
Boling Point | 704.1±60.0 °C(Predicted) |
Solubility | DMSO: ≥ 51 mg/mL |
Appearance | powder |
Color | white to beige |
pKa | 13.29±0.46(Predicted) |
Storage Condition | 2-8°C |
In vitro study | In the PPM1D-amplified MCF7 breast carcinoma cells, GSK2830371 increases the phosphorylation of multiple Wip1 substrates, including p53 (S15), Chk2 (T68), H2AX (S139) and ATM (S1981). GSK2830371 shows selective antiproliferative activity in a subset of lymphoid cell lines, all of which carry a wild-type TP53 allele. Furthermore co-treatment of doxorubicin and GSK2830371 results in a synergistic synergistic effect in DOHH2 and MX-1 tumor cells. In PPM1D amplified MCF7 Breast cancer cells, GSK2830371 increased multiple Wip1 substrates, including p53 (S15),Chk2 (T68),H2AX (S139) and ATM (S1981) phosphorylation. GSK2830371 exhibits selective anti-proliferative activity in a subset of lymphoid cell lines carrying the wild-type TP53 allele. In addition, doxorubicin and GSK2830371 co-treatment showed synergistic anti-proliferative effects in DOHH2 and MX-1 tumor cells. |
In vivo study | In vivo, GSK2830371 contributions of Chk2 (T68) and p53 (S15) and decreswip1 protein concentrations in DOHH2 tumors. GSK2830371 (150 mg/kg p.o.) also inhibit the growth of DOHH2 tumor Xeno graftvia inhibition of Wip1 In vivo, GSK2830371 increased the phosphorylation of Chk2 (T68) and p53 (S15), and reduced Wip1 protein concentration in DOHH2 tumors. GSK2830371 (150 mg/kg p.o.) also inhibited the growth of DOHH2 tumor xenografts by inhibiting Wip1. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.169 ml | 10.846 ml | 21.691 ml |
5 mM | 0.434 ml | 2.169 ml | 4.338 ml |
10 mM | 0.217 ml | 1.085 ml | 2.169 ml |
5 mM | 0.043 ml | 0.217 ml | 0.434 ml |