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WHI-P154

Cat. No. M3130
WHI-P154 Structure
Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 380 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.

Protocol
Cell Experiment
Cell lines U87, U737
Preparation method Seeding the cells into a 96-well plate at a density of 2.5×104 cells/well and incubating for 36 h at 37 ℃ before drug exposure. On the day of treatment, culture medium is carefully aspirated from the wells and replaced with fresh medium which contains the quinazoline compounds WHI-P154 at concentrations ranging from 0.1 μM to 250 μM. Using triplicate wells for each treatment. Incubating the cells with the compound for 24 hours to 36 hours at 37 ℃ in a humidified 5% CO2 atmosphere.10 μL of MTT (final concentration for each well, 0.5 mg/mL) is added, and the plate are incubated at 37 ℃ for 4 h. Than solubilized overnight at 37 ℃ in a solution containing 10% SDS in 0.01 M HCL. Mearsuring the absorbance of each well in a microplate reader at 570 nm.
Concentrations 0.1-250 μM
Incubation time 24-36 h
Animal Experiment
Animal models SCID Xenograft Model of Human Glioblastoma (U737)
Formulation Dissolved in PBS
Dosages 0.5 mg/kg or 1 mg/kg for 10 days
Administration 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 376.2
Formula C16H14BrN3O3
CAS Number 211555-04-3
Purity >98%
Solubility DMSO 60 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: WHI-P154 supplier, JAK, inhibitors

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