Home Protein Tyrosine Kinase c-RET inhibitor - Src inhibitor - S6 Kinase inhibitor AD80 For research use only.

AD80

AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.

AD80 Chemical Structure

AD80 Chemical Structure

CAS: 1384071-99-1

Selleck's AD80 has been cited by 7 publications

Purity & Quality Control

Batch: S851801 DMSO] 94 mg/mL] false] Ethanol] 94 mg/mL] false] Water] Insoluble] false Purity: 99.85%
99.85

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Biological Activity

Description AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.
Targets
Raf [2]
(Cell-free)		 Src [2]
(Cell-free)		 S6 Kinase [2]
(Cell-free)		 RET V804M [1]
(Cell-free assay)		 RET V804L [1]
(Cell-free assay)		 Click to View More Targets
0.4 nM 0.6 nM
In vitro
In vitro AD80 prevents the phosphorylation of RET as well as of extracellular signa-regulated kinase (ERK), AKT, and S6K at low nanomolar concentrations in kinesin family member 5B (KIF5B)-RET-expressing Ba/F3 cells. Treatment with AD80 results in up-regulation of genes that are typically repressed by active KRAS. On the contrary, genes that are activated by KRAS were down-regulated[1]. On the basis of in vitro human kinase profiles, AD80 and AD81 inhibit RET, RAF, SRC and S6K, with greatly reduced mTOR activity relative to AD57 and AD58. AD80 inhibits proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, probably through the induction of apoptosis[2].
Cell Research Cell lines LC-2/AD cells
Concentrations 0, 10, or 100 nM
Incubation Time 4 h
Method

Immunoblotting is performed in LC-2/AD cells treated with AD80, cabozantinib, or vandetanib (4 hours).
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-RET / RET / p-AKT / AKT / p-ERK / ERK / p-S6 / S6 28615362
In Vivo
In vivo AD80 is a highly potent RET inhibitor with a favorable pharmacokinetic profile in clinically relevant RET fusion-driven tumor models. AD80 potently shrinks RET-rearranged tumors in patient-derived xenografts. A pronounced reduction in phosphorylation of RET as well as AKT and ERK in tumors treated with AD80 (25 mg/kg) is observed but not in tumors treated with cabozantinib or vandetanib[1].
Animal Research Animal Models NSG mice
Dosages 12.5 to 25 mg/kg 
Administration oral gavage

Chemical lnformation & Solubility

Molecular Weight 473.43 Formula

C22H19F4N7O
CAS No. 1384071-99-1 SDF Download AD80 SDF
Smiles CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC=C(C=C3)NC(=O)NC4=C(C=CC(=C4)C(F)(F)F)F)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (198.55 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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