Idasanutlin (RG-7388)

Catalog No.S7205

Idasanutlin (RG-7388) Chemical Structure

Molecular Weight(MW): 616.48

Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.

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Biological Activity

Description Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.
Targets
Mdm2 [1]
(Cell-free assay)
6 nM
In vitro

Idasanutlin inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SJSA1 cells MkjBR5l1d3SxeHnjxsBie3OjeR?= M3fjU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNLW0FzIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIIC1N{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNUDPxE1? MWCyN|gxQDV2NR?=
HCT116 cells NXmwfZRZS3m2b4TvfIlkyqCjc4PhfS=> NXjWVHI5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJJA2OyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDifUBOXFRiYYPzZZktKEmFNUC9NE4xOSEQvF2= M4qzTVI{QDB6NUS1
SJSA1 cells MkTsVJJwdGmoZYLheIlwdiCjc4PhfS=> NHTnSW0yKGh? NIr6Vm1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPKV2EyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSYRWKGmwY3;ydI9z[XSrb36gZYZ1\XJiMTDodkBjgSCFbHnjb{1qXCCHZGWgTGNUKGG|c3H5JIlvKHC{ZYPlcoNmKG:oIEGwKUBpfW2jbjDz[ZJ2dSxiSVO1NF0xNjB2NTFOwG0> MYeyOFQ2PjR5Mh?=
SJSA1 cells M4LofGN6fG:2b4jpZ:Kh[XO|YYm= M{e4NVE3KGh? NHvpNVNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUlODMTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiBzNjDodpMh[nliRXTVJIlv[2:{cH;yZZRqd25iYYPzZZkhcW5icILld4Vv[2Vib3[gNVAmKGi3bXHuJJNmenWvLDDJR|UxRTBwMES1JO69VQ>? NEDyN5EzPDZyMU[0OC=>
RKO cells NHXRbYtEgXSxdH;4bYPDqGG|c3H5 NIPYWphEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTU09iY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGVicEWzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1yLkC3JO69VQ>? NYH5VZZTOjN6MEi1OFU>
MDA-MB-435 cells MV\DfZRwfG:6aXRCpIF{e2G7 Ml7pR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczDlfJBz\XO|aX7nJJA2OyCvdYThcpQh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYomgUXRVKGG|c3H5MEBKSzVyPUmuNUDPxE1? M4WxdlI{QDB6NUS1
SW480 cells M4\SVWN6fG:2b4jpZ:Kh[XO|YYm= MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTW|Q5OCClZXzsd{BmgHC{ZYPzbY5oKHB3MzDteZRidnRiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZpkhVVSWIHHzd4F6NCCLQ{WwQVE{NjNizszN M3fpe|I{QDB6NUS1

... Click to View More Cell Line Experimental Data

In vivo In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) causes tumor growth inhibition and regression. [1] In a SJSA xenograft model, Idasanutlin results in induction of apoptosis and antiproliferation. [2]

Protocol

Kinase Assay:

[1]

+ Expand

Biochemical Binding Affinity – HTRF Assay:

The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient.
Cell Research:

[1]

+ Expand
  • Cell lines: wt-p53 cancer cell lines (SJSA1, RKO, HCT116)
  • Concentrations: ~10 μM
  • Incubation Time: 24 hours
  • Method:

    Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Mice bearing SJSA human osteosarcoma xenografts
  • Formulation: Suspended in 1% Klucel LF/0.1% Tween 80
  • Dosages: ~50 mg/kg daily
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (162.21 mM)
Ethanol 8 mg/mL warmed (12.97 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
6.5mg/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 616.48
Formula

C31H29Cl2F2N3O4

CAS No. 1229705-06-9
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02828930 Completed Solid Tumors Hoffmann-La Roche September 8 2016 Phase 1
NCT03158389 Recruiting Glioblastoma Adult University Hospital Heidelberg|German Cancer Aid|German Cancer Research Center|National Center for Tumor Diseases Heidelberg May 7 2018 Phase 1|Phase 2
NCT02670044 Recruiting Leukemia Myeloid Acute Hoffmann-La Roche March 31 2016 Phase 1|Phase 2
NCT02633059 Recruiting Loss of Chromosome 17p|Recurrent Plasma Cell Myeloma Mayo Clinic|National Cancer Institute (NCI) December 30 2015 Phase 1|Phase 2
NCT02545283 Recruiting Leukemia Myeloid Acute Hoffmann-La Roche December 30 2015 Phase 3
NCT03362723 Active not recruiting Solid Tumors Hoffmann-La Roche November 27 2017 Phase 1

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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Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID