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LB-100

Cat. No. M8990
LB-100 Structure
Size Price Availability Quantity
5mg USD 145 In stock
10mg USD 250 In stock
50mg USD 830 In stock
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Quality Control
  • Current batch:
  • Purity >95%
  • COA
  • MSDS
Biological Activity

LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells. LB-100 increases concentration of doxorubicin within cells (2.5 fold to control) and sensitizes tumor cells to the cytotoxicity of doxorubicin. LB-100 increaseds VEGF secretion, and thus enhances HIF-1α-VEGF mediated angiogenesis.

In vivo, LB-100 (2 mg/kg, i.p.) decreases in a time-dependent manner the activity of PP2A in xenografts and livers in nude mice. The combination of doxorubicin (1.5 kg/mL, every other day) and LB-100 (2 mg/kg, every other day) significantly slows the growth of tumors with reduction of tumor volume in two animals with no effects on tumor growth in animals treated with single agents.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 268.31
Formula C13H20N2O4
CAS Number 1026680-07-8; 1632032-53-1
Purity >95%
Solubility Water ≥ 40 mg/mL
Storage at -20°C
References

Inhibition of protein phosphatase 2A enhances cytotoxicity and accessibility of chemotherapeutic drugs to hepatocellular carcinomas.
Bai XL, et al. Mol Cancer Ther. 2014 Aug;13(8):2062-72. PMID: 24867249.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LB-100 supplier, inhibitors

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