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| Size | Price | Stock |
|---|---|---|
| 5mg | $70 | 3-6 Days |
| 10mg | $115 | 3-6 Days |
| 25mg | $190 | 3-6 Days |
| 50mg | $320 | 3-6 Days |
| 100mg | $500 | 3-6 Days |
| 250mg | $925 | 3-6 Days |
| 500mg | $1450 | 3-6 Days |
: Cat #: V1901 CAS #: 1632032-53-1 Purity ≥ 98%
Description: LB-100 (LB100) is a water soluble small-molecular protein phosphatase 2A (PP2A) inhibitor with anticancer activity. It inhibits PP2A 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.
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| Molecular Weight (MW) | 268.31 |
|---|---|
| Molecular Formula | C13H20N2O4 |
| CAS No. | 1632032-53-1 |
| 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: N/A | |
| Synonyms | LB100; LB 100; LB-100 |
| Protocol | 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 a |
|---|---|---|
| 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 | BALB/c nude mice are injected subcutaneously in the right flank with 1×106 Huh-7 cells suspended in 200 μL PBS per mouse. After a tumor volume of 100 to 200 mm3 is reached, tumor-bearing mice are randomLy allocated to four groups: control group, doxorubicin/cisplatin group, LB-100 group, and doxorubicin/cisplatin plus LB-100 group. For the doxorubicin plus LB-100 study (n=6 to 8), doxorubicin and LB-100 are injected i.p. at 1.5 and 2 mg/kg, respectively, on alternate days for a total of 16 days. For the cisplatin plus LB-100 study (n=8 to 10), cisplatin and LB-100 are injected at 3 and 2.5 mg/kg, i.p., respectively; cisplatin is injected every 4 days and LB-100 is used every other day for 16 days. Control mice are injected with DMSO (in the doxorubicin plus LB-100 group) or PBS (in the cisplatin plus LB-100 group) on the same schedule as the drug-treated animals. Tumor size is monitored every 3 or 4 days, and is calculated by the formula: tumor volume=length × width × height/2. All mice are sacrificed at day 16, and xenografts are obtained, weighed, and fixed with 10% formaldehyde. |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.7270 mL | 18.6352 mL | 37.2703 mL | 74.5406 mL |
| 5mM | 0.7454 mL | 3.7270 mL | 7.4541 mL | 14.9081 mL |
| 10mM | 0.3727 mL | 1.8635 mL | 3.7270 mL | 7.4541 mL |
| 20mM | 0.1864 mL | 0.9318 mL | 1.8635 mL | 3.7270 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.