1. MAPK/ERK Pathway
    Protein Tyrosine Kinase/RTK
  2. Raf
    Src
    Ribosomal S6 Kinase (RSK)
    RET
  3. AD80

AD80 

Cat. No.: HY-101963 Purity: 99.46%
Handling Instructions

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

For research use only. We do not sell to patients.

AD80 Chemical Structure

AD80 Chemical Structure

CAS No. : 1384071-99-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 219 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 210 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
25 mg USD 720 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All Raf Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

IC50 & Target[1]

RAF

 

RET

 

SRC

 

In Vitro

AD80 is a polypharmacological agent with an optimal balance of activity against Ret, Raf, Src, Tor and S6K that show high efficacy with very low toxicity. AD80 and AD81 inhibits RET, RAF, SRC and S6K, with greatly reduced mTOR activity relative to AD57 and AD58.AD80 is optimal for Ras–Erk pathway inhibition. AD80 inhibits proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, probably through the induction of apoptosis. Immunoblot analysis demonstrates potent downregulation of phosphorylated Ret and several downstream biomarkers within these cells[1]. AD80 coordinately inhibits S6K1 together with the TAM family tyrosine kinase AXL.AD80 avoides S6K1 phosphorylation and mTOR co-association, resulting in durable suppression of S6K1-induced signaling and protein synthesis[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral administration of either AD80 or AD81 results in a notable 70-90% of animals developing to adulthood in Drosophila ptc>dRetMEN2Bmodel, a considerable improvement over the efficacy observed with AD57. AD80 also promotes enhanced tumour growth inhibition and reduces body-weight modulation relative to vandetanib in a mouse xenograft model[1]. AD80 rescues 50% of mice transplanted with PTEN-deficient leukemia cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

473.43

Formula

C₂₂H₁₉F₄N₇O

CAS No.

1384071-99-1

SMILES

O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C3=NN(C(C)C)C4=NC=NC(N)=C43)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (316.84 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1122 mL 10.5612 mL 21.1224 mL
5 mM 0.4224 mL 2.1122 mL 4.2245 mL
10 mM 0.2112 mL 1.0561 mL 2.1122 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

MZ-CRC-1 (MEN2B) and TT (MEN2A) cells are treated with AD80 (0.2 nM to 20 μM) for 7 days and cell viability is quantitated by MTT assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice:
Mice showing established growing tumors are separated into vehicle or drug treatment groups. A similar range of tumor sizes is selected for each experiment (vehicle vs AD57; vehicle vs AD80 vs Vandetanib). Vehicle, AD57 (20 mg/kg), AD80 (30 mg/kg), or Vandetanib (50mg/kg) are administered by oral gavage (PO; per os or by mouth) once daily, five times a week. Tumor and body weight measurements are performed 3 times a week[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.46%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

AD80AD 80AD-80RafSrcRibosomal S6 Kinase (RSK)RETRaf kinasesS6KInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AD80
Cat. No.:
HY-101963
Quantity:
MCE Japan Authorized Agent: