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Danusertib (PHA-739358)

Pan-aurora kinase inhibitor

Danusertib (PHA-739358)

Catalog No. A4116
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $110.00 In stock
10mg $190.00 In stock
50mg $590.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Danusertib (PHA-739358)

Related Biological Data

Danusertib (PHA-739358)

Related Biological Data

Danusertib (PHA-739358)

Biological Activity

Description Danusertib (PHA-739358) is an inhibitor of Aurora kinase for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc
Targets Aurora A/B/C Bcr-Abl c-RET FGFR TrkA  
IC50 13 nM/79 nM/61 nM 25nM 31 nM 47 nM 30 nM  

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Chemical Properties

Cas No. 827318-97-8 SDF Download SDF
Synonyms 5-Amido-pyrrolopyrazole 9d
Chemical Name N-[5-[(2R)-2-methoxy-2-phenylacetyl]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide
Canonical SMILES CN1CCN(CC1)C2=CC=C(C=C2)C(=O)NC3=NNC4=C3CN(C4)C(=O)C(C5=CC=CC=C5)OC
Formula C26H30N6O3 M.Wt 474.55
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

Danusertib (previously known as PHA-739358), a 3-aminopyrazole derivative identified during the development of the pyrrolopyrazole sub-series, is a potent small-molecule inhibitor of aurora kinases family members with a dominant inhibition for aurora B kinase (ABK). This pan-aurora kinases inhibitor is also able to inhibit several tyrosine kinases, including T315I mutant, Ret, Trk-A and fibroblast growth factor receptor-1 (FGFR-1), which are involved in multiple malignancies, such as chronic myelogenous leukemia (CML), acute lymphoblastic leukemia (ALL), thyroid prostate and breast carcinoma. Thus, in many previous studies, danusertib exhibits remarkable antitumor activity in a number of different xengorafts, spontaneous, and transgenic animal tumor models with a favorable pharmacokinetic and safety profile.

Reference

Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J. PHA-739358, a potent inhibitor of aurora kinases with a selecyive target inhibiton profile relevant to cancer. Mol Cancer Ther 2007; 6(12 Pt 1): 3158-3168