product name LB-100
Description: LB-100 is a water soluble small-molecular protein phosphatase 2A(PP2A) inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells. By using CCK-8 assays, LB-100 showed dose-dependent inhibition of cell growth in both cell lines. The IC50 of LB-100 was 0.85 μM and 3.87 μM in BxPc-3 and Panc-1, respectively. While the IC50 of doxorubicin was 2.3 μM and 1.7 μM in BxPc-3 and Panc-1, respectively, LB-100 did not synergize with doxorubicin in both cell lines. LB-100 treatment reduced PP2A activity by 30–50% in different pancreatic cell lines. LB-100 treatment increased the relative concentration of doxorubicin by up to 2.5 fold compared to cells not exposed to LB-100. LB-100 significantly enhanced inhibition of HCC by doxorubicin and cisplatin in vitro and in vivo in a PP2A-dependent way, while having little inhibitory activity when used alone.
References: Cancer Lett. 2014 Dec 28;355(2):281-7; Mol Cancer Ther. 2014 Aug;13(8):2062-72.
268.31
Formula
C13H20N2O4
CAS No.
1026680-07-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: < 2.9 mg/mL
Water: ≥ 48 mg/mL
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: By using CCK-8 assays, LB-100 showed dose-dependent inhibition of cell growth in both cell lines. The IC50 of LB-100 was 0.85 μM and 3.87 μM in BxPc-3 and Panc-1, respectively. While the IC50 of doxorubicin was 2.3 μM and 1.7 μM in BxPc-3 and Panc-1, respectively, LB-100 did not synergize with doxorubicin in both cell lines. LB-100 treatment reduced PP2A activity by 30–50% in different pancreatic cell lines. LB-100 treatment increased the relative concentration of doxorubicin by up to 2.5 fold compared to cells not exposed to LB-100. LB-100 significantly enhanced inhibition of HCC by doxorubicin and cisplatin in vitro and in vivo in a PP2A-dependent way, while having little inhibitory activity when used alone. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | LB-100 injection resulted in rapid blood flow at the surface of tumors in mice. LB-100 promoted vascular endothelial growth factor secretion and vasculogenic mimicry, associated with increased microvessel density and blood perfusion of tumor cell xenografts. LB-100 also enhanced paracellular endothelial permeability to Evans Blue dye and doxorubicin in vivo and in vitro, presumably by altering vascular endothelial-cadherin contact between cells. |
| Animal model | |
| Formulation & Dosage | |
| References | Cancer Lett. 2014 Dec 28;355(2):281-7; Mol Cancer Ther. 2014 Aug;13(8):2062-72. |
