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AD80

Chemical Structure : AD80

CAS No.: 1384071-99-1

AD80 (RET inhibitor AD80)

Catalog No.: PC-35268Not For Human Use, Lab Use Only.

AD80 is a multikinase inhibitor that shows strong activity against human RET (IC50=4 nM), BRAF, S6K, and SRC, but has greatly reduced mTOR activity.

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Biological Activity

AD80 is a multikinase inhibitor that shows strong activity against human RET (IC50=4 nM), BRAF, S6K, and SRC, but has greatly reduced mTOR activity.
AD80 inhibits S6K1 and suppress oncogenic function downstream of a transforming mutant of the receptor tyrosine kinase Ret.
AD80 demonstrates selective cytotoxicity for PTEN-deficient cells established S6K1 as part of a kinase targeting portfolio for in vitro and in vivo cytotoxic therapy of PTEN-deficient cancers.
AD80 inhibits proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, also promotes enhanced tumour growth inhibition and reduced body-weight modulation relative to vandetanib in a mouse xenograft model.

Physicochemical Properties

M.Wt 473.436
Formula C22H19F4N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[4-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[2-fluoro-5-(trifluoromethyl)phenyl]urea

References

1. Plenker D, et al. Sci Transl Med. 2017 Jun 14;9(394). pii: eaah6144.

2. Liu H, et al. Cell Rep. 2017 Feb 28;18(9):2088-2095.

3. Dar AC, et al. Nature. 2012 Jun 6;486(7401):80-4.

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