Danusertib (PHA-739358)

For research use only.

Catalog No.S1107

25 publications

Danusertib (PHA-739358) Chemical Structure

CAS No. 827318-97-8

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.

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Selleck's Danusertib (PHA-739358) has been cited by 25 publications

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Biological Activity

Description Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Targets
Aurora A [1]
(Cell-free assay)
Abl [1]
(Cell-free assay)
RET [1]
(Cell-free assay)
TrkA [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
13 nM 25 nM 31 nM 31 nM 47 nM
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. [1] Increasing concentrations of Danusertib produces a dose-dependent reduction of cell growth after 48 hours in BCR-ABL-positive (K562, BV173) and BCR-ABL-negative (HL60) cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780 cells MofaVJJwdGmoZYLheIlwdiCjc4PhfS=> M{PtbmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRVI4QDBiY3XscJMtKEmFNUC9Nlghdk1? NF;3TFgyPzF{NUK3PS=>
HCT116 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 M33PPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgTGNVOTF4IHPlcIx{NCCLQ{WwQVMyKG6P M2\KZVE4OTJ3Mke5
human HCT116 cells MlzsVJJwdGmoZYLheIlwdiCjc4PhfS=> MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{BDemSXIHnuZ49zeG:{YYTpc44h[W[2ZYKgO|IhcHK|LDDJR|UxRTNzIH7N MVixPVMzODR6OR?=
HCT116 cells MnX5SpVv[3Srb36gZZN{[Xl? MmfGR4VtdCCleXPs[UBienKnc4SgbY4hUEOWMUG2JINmdGy|IHL5JIFk[3WvdXzheIlwdiCjdDDHNk9OKHCqYYPlMEBGSzVyPUiwJI5O M{SyVVE4OTJ3Mke5
MCF7 cells NYLhdHI{WHKxbHnm[ZJifGmxbjDhd5NigQ>? NYGyRYlCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBOS0Z5IHPlcIx{NCCLQ{WwQVgxKG6P NWX6d3l2OTdzMkWyO|k>
HeLa cells M1XVcXBzd2yrZnXyZZRqd25iYYPzZZk> MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFjlUIEh[2WubIOsJGlEPTB;MD6xOEDPxE1? NGHVOWkyPzF{NUK3PS=>
human MOLT4 cells NUSzcIJKS3m2b4TvfIlkyqCjc4PhfS=> NInkPWJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOV0yWNDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHHmeIVzKDRiZHH5d{BjgSCFZXzsJHRqfGW{IFLseYUh\W6mLYDvbY51KGG|c3H5MEBGSzVyPUCuNVUh|ryP Mk\lNlI5QDl3NkG=
human HepG2 cells MnXDR5l1d3SxeHnjxsBie3OjeR?= NUTHdppYS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiVFO1NF01KM7:TR?= MVWyOFkyODd4Nh?=
human A2780 cells MliwVJJwdGmoZYLheIlwdiCjc4PhfS=> MkC4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25ib3[gOG4hTE6DLDDJR|UxRTJ6IN88US=> M{DOcVE6OzJyNEi5
HCT116 cells NVvyO3F4TnWwY4Tpc44h[XO|YYm= MoTWTY5pcWKrdHnvckBw\iCqaYP0c45mKGh|IIDoc5NxcG:{eXzheIlwdiCrbjDIR3QyOTZiY3XscJMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M2jPeFE4OTJ3Mke5

... Click to View More Cell Line Experimental Data

In vivo 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. [1] Danusertib significantly inhibits proliferation of K562 cells and virtually suppressed tumor growth during the 10-day treatment period. [3]

Protocol

Kinase Assay:[1]
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Biochemical kinase Assays:

The Km values for ATP and the specific substrate are initially determined, and each assay is then run at optimized ATP (2Km) and substrate (5Km) concentrations. This setting enabled direct comparison of IC50 values of Danusertib across the applied kinase selectivity screening panel for the evaluation of the selectivity profile.
Cell Research:[3]
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  • Cell lines: CD34+ cells
  • Concentrations: 5 μM
  • Incubation Time: 5 days
  • Method: For short-term expansion assays, 1 × 103 CD34+ cells are plated in triplicates in 96-well plates containing 100 μL of serum-free medium per well supplemented with human stem-cell factor (100 ng/mL), human Flt-3 Ligand (100 ng/mL), human thrombopoietin (50 ng/mL), human interleukin-3 and -6 (IL-3 and IL-6, respectively, both 20 ng/mL), and granulocyte colony-stimulating factor (20 ng/mL) along with Danusertib at the indicated concentrations. After 5 days, an additional 100 μL of cytokine and Danusertib containing medium are added. Cell numbers within each individual well are estimated on days 3, 6, and 9 or on days 3, 6, and 12 for healthy donor samples.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: Female SCID mice
  • Dosages: 15 mg/kg
  • Administration: Intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 95 mg/mL (200.18 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 474.55
Formula

C26H30N6O3

CAS No. 827318-97-8
Storage powder
in solvent
Synonyms N/A
Smiles CN1CCN(CC1)C2=CC=C(C=C2)C(=O)NC3=NNC4=C3CN(C4)C(=O)C(C5=CC=CC=C5)OC

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID