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AD80

Catalog No. T4301 CAS 1384071-99-1

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

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AD80, CAS 1384071-99-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
5 mg	In stock	$ 93.00
10 mg	In stock	$ 148.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 488.00
100 mg	In stock	$ 716.00
500 mg	In stock	$ 1,480.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 100%

Purity: 99.9%

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Description	AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
Targets&IC50	RET (V804M):0.4 nM, RET (V804L):0.6 nM
In vitro	AD80 and AD81 effectively inhibit key signaling molecules (RET, RAF, SRC, S6K) with significantly diminished mTOR activity compared to AD57 and AD58. Specifically, AD80 stands out for its proficient inhibition of the Ras–Erk pathway, showcasing a well-balanced polypharmacological profile that targets Ret, Raf, Src, Tor, and S6K, yielding high efficacy with minimal toxicity. Furthermore, AD80 demonstrates potent anti-proliferative effects on MZ-CRC-1 and TT thyroid cancer cells in vitro, likely mediated by triggering apoptosis. Additionally, AD80 uniquely suppresses S6K1 in conjunction with inhibiting the TAM family tyrosine kinase AXL, preventing S6K1 phosphorylation and its association with mTOR. This leads to a sustained inhibition of S6K1-driven signaling and protein synthesis, underscoring its therapeutic potential.
In vivo	AD80 significantly improves survival rates, rescuing 50% of mice transplanted with PTEN-deficient leukemia cells. When administered orally, both AD80 and AD81 remarkably allow 70-90% of Drosophila ptc>dRetMEN2B model animals to reach adulthood, surpassing the effectiveness of AD57. Furthermore, AD80 demonstrates superior tumor growth inhibition and minimizes body-weight fluctuations compared to vandetanib in a mouse xenograft model.
Cell Research	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.
Animal Research	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 (50 mg/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.

Molecular Weight	473.43
Formula	C22H19F4N7O
CAS No.	1384071-99-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL

References and Literature

1. Dar AC, et al. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology.Nature. 2012 Jun 6;486(7401):80-4. 2. Liu H, et al. Pharmacologic Targeting of S6K1 in PTEN-Deficient Neoplasia.Cell Rep. 2017 Feb 28;18(9):2088-2095. 3. Carlos J A E G, Lima K, Costa-Lotufo L V, et al. AD80, a multikinase inhibitor, exhibits antineoplastic effects in acute leukemia cellular models targeting the PI3K/STMN1 axis[J]. Investigational New Drugs. 2021: 1-11.

Citations

1. de Almeida L C, Carlos J A E G, Rezende-Teixeira P, et al. AD80, a multikinase inhibitor, as a potential drug candidate for colorectal cancer therapy. Life Sciences. 2022: 120911. 2. Carlos J A E G, Lima K, Costa-Lotufo L V, et al. AD80, a multikinase inhibitor, exhibits antineoplastic effects in acute leukemia cellular models targeting the PI3K/STMN1 axis. Investigational New Drugs. 2021 Aug;39(4):1139-1149. doi: 10.1007/s10637-021-01066-w. Epub 2021 Jan 21. 3. Carlos J A E G, Lima K, Costa-Lotufo L V, et al. AD80, a multikinase inhibitor, exhibits antineoplastic effects in acute leukemia cellular models targeting the PI3K/STMN1 axis. Investigational New Drugs. 2021 Aug;39(4):1139-1149. doi: 10.1007/s10637-021-01066-w. Epub 2021 Jan 21. 4. Lima K, de Miranda L B L, Del Milagro Bernabe Garnique A, et al.The Multikinase Inhibitor AD80 Induces Mitotic Catastrophe and Autophagy in Pancreatic Cancer Cells.Cancers.2023, 15(15): 3866.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Ovarian Cancer Compound Library NO PAINS Compound Library Antidepressant Compound Library Anti-Breast Cancer Compound Library Bioactive Compounds Library Max Kinase Inhibitor Library Glycolysis Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

AD80 1384071-99-1 Angiogenesis Apoptosis MAPK PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Raf c-RET Src S6 Kinase AD 80 Inhibitor inhibit Raf kinases AD-80 Ribosomal S6 Kinase (RSK) S6K RET inhibitor

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