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AMG-47a

Cat. No. M7569
AMG-47a  Structure
Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 260 In stock
25mg USD 600 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AMG-47a displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 μM, AMG-47a effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.

Protocol
Cell Experiment
Cell lines HeLa cells
Preparation method Cells were treated with varying concentrations of AMG-47a, Ponatinib, and Torin-1. Media and compound were refreshed after 3 days on cells being treated for 5 days.
Concentrations 1 uM
Incubation time 48-h
Animal Experiment
Animal models
Formulation
Dosages
Administration
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 535.56
Formula C29H28F3N5O2
CAS Number 882663-88-9
Purity >98%
Solubility 34 mg/mL in DMSO
Storage at -20°C
References

A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein.
Carver J, et al. PLoS One. 2014 Aug 5;9(8):e103836. PMID: 25093678.

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  Catalog
Abmole Inhibitor Catalog 2017




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