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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 120 In-stock
Solution
10 mM * 1 mL in DMSO USD 120 In-stock
Solid
5 mg USD 115 In-stock
10 mg USD 185 In-stock
25 mg USD 370 In-stock
50 mg USD 590 In-stock
100 mg USD 950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • 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]

p70S6K

 

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].

MedChemExpress (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].

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

Molecular Weight

473.43

Formula

C22H19F4N7O

CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (105.61 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.88%

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1122 mL 10.5612 mL 21.1224 mL 52.8061 mL
5 mM 0.4224 mL 2.1122 mL 4.2245 mL 10.5612 mL
10 mM 0.2112 mL 1.0561 mL 2.1122 mL 5.2806 mL
15 mM 0.1408 mL 0.7041 mL 1.4082 mL 3.5204 mL
20 mM 0.1056 mL 0.5281 mL 1.0561 mL 2.6403 mL
25 mM 0.0845 mL 0.4224 mL 0.8449 mL 2.1122 mL
30 mM 0.0704 mL 0.3520 mL 0.7041 mL 1.7602 mL
40 mM 0.0528 mL 0.2640 mL 0.5281 mL 1.3202 mL
50 mM 0.0422 mL 0.2112 mL 0.4224 mL 1.0561 mL
60 mM 0.0352 mL 0.1760 mL 0.3520 mL 0.8801 mL
80 mM 0.0264 mL 0.1320 mL 0.2640 mL 0.6601 mL
100 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5281 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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