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AD80

Cat. No. M10375
AD80 Structure
Synonym:

AD-80

Size Price Availability Quantity
2mg USD 100  USD100 In stock
5mg USD 200  USD200 In stock
10mg USD 330  USD330 In stock
50mg USD 1100  USD1100 In stock
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Quality Control & Documentation
Biological Activity

AD80 is a multikinase inhibitor, it potently targets human RET, BRAF, S6K, and SRC. AD80 inhibits proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, probably through the induction of apoptosis. 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. 

In vivo, 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. AD80 rescues 50% of mice transplanted with PTEN-deficient leukemia cells.

Chemical Information
Molecular Weight 473.43
Formula C22H19F4N7O
CAS Number 1384071-99-1
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jorge Antonio Elias Godoy Carlos, et al. Invest New Drυgs. AD80, a multikinase inhibitor, exhibits antineoplastic effects in acute leukemia cellular models targeting the PI3K/STMN1 axis

[2] Hongqi Liu, et al. Cell Rep. Pharmacologic Targeting of S6K1 in PTEN-Deficient Neoplasia

[3] Arvin C Dar, et al. Nature. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology

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  Catalog
Abmole Inhibitor Catalog




Keywords: AD80, AD-80 supplier, RET, inhibitors, activators


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