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Signaling Pathway

Danusertib

HY-10179

(PHA-739358; PHA739358; PHA 739358)

Danusertib

Danusertib Chemical Structure

Danusertib (PHA-739358) is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $190 In-stock
50 mg $590 In-stock
100 mg $850 Backordered
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €119 In-stock
5 mg €108 In-stock
10 mg €186 In-stock
50 mg €578 In-stock
100 mg €833 Backordered
200 mg Get quote
500 mg Get quote

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Product name: Danusertib
Cat. No.: HY-10179

Danusertib Data Sheet

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    Purity: 99.73%

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Biological Activity of Danusertib

Danusertib (PHA-739358) is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
IC50 Value: 13  nM(Aurora A); 79 nM(Aurora B); 61 nM(Aurora C)
Target: Aurora Kinase
in vitro: Danusertib inhibits the activities of other kinases such as FGFR1, Abl, Ret and Trka, with IC50 of 47 nM, 25 nM, 31 nM and 31 nM, respectively. In a cell assay, after treatment of wild-type and p53-deficient MEFs with Danusertib, the wild-type cells undergo an arrest in mitosis (4N) that is maintained for up to 48 h. The p53-deficient cells on the other hand do not arrest at the 4N DNA stage, but continues with additional rounds of DNA synthesis to become >8N. Treatment with Danusertib results in an increase in p53 protein levels and an associated increase in p21 protein, which is known to be transcriptionally regulated by p53.
in vivo: Danusertib significantly inhibits proliferation of K562 cells and virtually suppressed tumor growth during the 10-day treatment period. Administration of 25 mg/kg Danusertib (b.d. i.v.) to HL-60 xenograft rats results in 75% inhibition of tumor growth with complete regression in one animal. Danusertib results in biomarker modulation accompanied by inhibition of tumor growth. This is compatible with an expected mechanism of action of aurora kinase inhibition.

Chemical Information

M.Wt 474.55 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C26H30N6O3
CAS No 827318-97-8
Solvent & Solubility

DMSO ≥90mg/mL Water <1.2mg/mL Ethanol ≥30mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.1073 mL 10.5363 mL 21.0726 mL
5 mM 0.4215 mL 2.1073 mL 4.2145 mL
10 mM 0.2107 mL 1.0536 mL 2.1073 mL

Clinical Information of Danusertib

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Danusertib Jonsson Comprehensive Cancer Center Chronic myelocytic leukemia 31-MAR-07 Phase 2 03-NOV-10
Nerviano Medical Sciences Srl Hormone refractory prostate cancer 30-SEP-07 30-APR-11 Phase 2 10-MAY-13
Nerviano Medical Sciences Srl Multiple myeloma 31-OCT-08 30-SEP-10 Phase 2 08-OCT-09

References on Danusertib

Inhibitor Kit

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