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PIK-90

Cat. No. M1896
PIK-90 Structure
Size Price Availability Quantity
10mg USD 87 In stock
50mg USD 270 In stock
100mg USD 430 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PIK-90 is a novel and potent PI3K inhibitor with IC50 values of 11 nM, 350 nM, 18 nM and 58 nM for p110α, p110β, p110γ and p110δ respectively. Phosphoinositide 3-kinases (PI3Ks) are among the most frequently activated signaling pathways in cancer. Inhibition with p110alpha inhibitor PIK-90 resulted in a significant reduction of chemotaxis and actin polymerization to CXCL12 and reduced migration beneath MSC (pseudoemperipolesis). In suspension and MSC cocultures, PIK-90 was potent inducers of CLL cell apoptosis.

Protocol
Cell Experiment
Cell lines LN229:EGFR (PTENwt) and U87:EGFR (PTENmt) cells
Preparation method Cell proliferation assay and flow cytometry. For viability, 105 cells were seeded in 12-well plates in the presence of erlotinib, PI-103, PIK-90, rapamycin, erlotinib plus PIK-90, erlotinib plus rapamycin, erlotinib plus PIK-90, and rapamycin or erlotinib plus PI-103 for 72 h. Cell viability was determined using a WST-1 assay (Roche Molecular Biochemicals).
Concentrations 0, 0.1, 0.5, 1µM
Incubation time 72h
Animal Experiment
Animal models Human primary GBM43 cells female BALB/c nu/nu mice bearing xenografts model
Formulation DMSO:H20
Dosages 40 mg/kg
Administration daily i.p.
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 351.36
Formula C18H17N5O3
CAS Number 677338-12-4
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Proc Natl Acad Sci U S A (2012). Figure 1.PIK-90
Method apoptosis assay
Cell Lines PTENWT and PTENMT glioma cell lines
Concentrations 0.5 μM
Incubation Time 24 h
Results Like PIK-90, PI-103, and LY294002, PIK-75 could block phosphorylation of Akt
Rating
References

Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach.
Niedermeier M, et al. Blood. 2009 May 28;113(22):5549-57. PMID: 19318683.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PIK-90 supplier, PI3K, inhibitors

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