AD80

Catalog No.S8518

AD80 Chemical Structure

Molecular Weight(MW): 473.43

AD80, a multikinase inhibitor, shows strong activity against human 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.

Size Price Stock Quantity  
USD 147 In stock
USD 270 In stock
USD 897 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective c-RET Inhibitors

Biological Activity

Description AD80, a multikinase inhibitor, shows strong activity against human 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)
0.4 nM 0.6 nM
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].

Assay
Methods Test Index PMID
Western blot
p-RET / RET / p-AKT / AKT / p-ERK / ERK / p-S6 / S6 ; 

PubMed: 28615362     


B) Immunoblotting results of KIF5B-RET rearranged Ba/F3 cells after treatment are displayed (4h). CAB: cabozantinib, VAN: vandetanib  

28615362
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].

Protocol

Cell Research:

[1]

+ Expand
  • 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).


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: NSG mice
  • Formulation: 5% DMSO and 40% PEG400 in saline
  • Dosages: 12.5 to 25 mg/kg 
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (198.55 mM)
Ethanol 94 mg/mL (198.55 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 473.43
Formula

C22H19F4N7O

CAS No. 1384071-99-1
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

c-RET Signaling Pathway Map

Related c-RET Products0

Tags: buy AD80 | AD80 supplier | purchase AD80 | AD80 cost | AD80 manufacturer | order AD80 | AD80 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID