| CAS NO: | 1632032-53-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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: N/A | |
| Other info | Chemical Name:
3-[(4-Methylpiperazin-1-yl)carbonyl]-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid InChi Key: JUQMLSGOTNKJKI-UHFFFAOYSA-N InChi Code: InChI=1S/C13H20N2O4/c1-14-4-6-15(7-5-14)12(16)10-8-2-3-9(19-8)11(10)13(17)18/h8-11H,2-7H2,1H3,(H,17,18) SMILES Code: O=C(C1C(O2)CCC2C1C(N3CCN(C)CC3)=O)O |
| Synonyms | LB100; LB 100; LB-100 |
| 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. |
| Formulation & Dosage | 2 mg/kg |
| References | Cancer Lett. 2014 Dec 28;355(2):281-7; Mol Cancer Ther. 2014 Aug;13(8):2062-72. |
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