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Atiprimod (dimaleate)

Atiprimod (Azaspirane) (dimaleate) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) [1][2][3][4][5][6].

Product Specifications

CAS Number

183063-72-1

Product Name Alternative

Azaspirane (dimaleate) ; SKF 106615-12 (dimaleate) ; SKF 106615A12 (dimaleate)

UNSPSC

12352005

Target

Apoptosis; Atg8/LC3; Autophagy; Caspase; Interleukin Related; JAK; p62; Reactive Oxygen Species (ROS) ; STAT

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; Metabolic Enzyme/Protease; NF-κB; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/atiprimod-dimaleate.html

Smiles

CCCC(CC1)(CCC)CCC21CCN(CCCN(CC)CC)C2.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O

Molecular Formula

C30H52N2O8

Molecular Weight

568.74

References & Citations

[1]Coker-Gurkan A, et al. Atiprimod induce apoptosis in pituitary adenoma: Endoplasmic reticulum stress and autophagy pathways. J Cell Biochem. 2019 Dec;120 (12) :19749-19763. |[2]Coker-Gurkan A, et al Atiprimod triggered apoptotic cell death via acting on PERK/eIF2α/ATF4/CHOP and STAT3/NF-ΚB axis in MDA-MB-231 and MDA-MB-468 breast cancer cells. Mol Biol Rep. 2021 Jun;48 (6) :5233-5247. |[3]Faderl S, et al. Atiprimod blocks phosphorylation of JAK-STAT and inhibits proliferation of acute myeloid leukemia (AML) cells. Leuk Res. 2007 Jan;31 (1) :91-5.|[4]Wang M, et al. Atiprimod inhibits the growth of mantle cell lymphoma in vitro and in vivo and induces apoptosis via activating the mitochondrial pathways. Blood. 2007 Jun 15;109 (12) :5455-62. |[5]Hamasaki M, et al. Azaspirane (N-N-diethyl-8,8-dipropyl-2-azaspiro [4.5] decane-2-propanamine) inhibits human multiple myeloma cell growth in the bone marrow milieu in vitro and in vivo. Blood. 2005 Jun 1;105 (11) :4470-6. |[6]Quintás-Cardama A, et al. Preclinical characterization of atiprimod, a novel JAK2 AND JAK3 inhibitor. Invest New Drugs. 2011 Oct;29 (5) :818-26.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 2

Frequently Asked Questions

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