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Danusertib (PHA-739358)

Danusertib (PHA-739358)

Catalog Number:
L002369028APE
Mfr. No.:
APE-A4116
Price:
$292
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      • Overview

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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.

      • Properties
        • Alternative Name
          5-Amido-pyrrolopyrazole 9d; N-[5-[(2R)-2-methoxy-2-phenylacetyl]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide
          CAS Number
          827318-97-8
          Molecular Formula
          C26H30N6O3
          Molecular Weight
          474.55
          Appearance
          A solid
          Purity
          99.39%
          Solubility
          ≥23.75 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference

        • 1. Wang R, Yang JF, et al. "Bromodomain-Containing Protein BRD4 Is Hyperphosphorylated in Mitosis." Cancers (Basel). 2020;12(6):E1637. PMID:32575711
          2. Wang H, Tian L, et al. "The Osteogenic Niche Is a Calcium Reservoir of Bone Micrometastases and Confers Unexpected Therapeutic Vulnerability." Cancer Cell. 2018 Nov 12;34(5):823-839.e7. PMID:30423299
          3. Wang H, Tian L, et al. "Bone-in-culture array as a platform to model early-stage bone metastases and discover anti-metastasis therapies." Nat Commun. 2017 Apr 21;8:15045. PMID:28429794

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