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 NWq0XIc2S3m2b4TvfIlkyqCjc4PhfS=> NFWze45EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUlODMTDj[YxteyCneIDy[ZN{cW6pIIfpcIQhfHmyZTDwOVMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYomgUXRVKGG|c3H5MEBKSzVyPUCuNFEh|ryP MmO1NlM5ODh3NEW=
HCT116 cells Mn20R5l1d3SxeHnjxsBie3OjeR?= NFHCXmVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgdFU{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAyKM7:TR?= M2TUblI{QDB6NUS1
SJSA1 cells NFnXOJVRem:uaX\ldoF1cW:wIHHzd4F6 M{LocFEhcA>? M4PkWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1rTRVEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDF[HUhcW6lb4Lwc5JifGmxbjDh[pRmeiBzIHjyJIJ6KEOuaXPrMYlVKEWmVTDIR3Mh[XO|YYmgbY4heHKnc3XuZ4Uhd2ZiMUClJIh2dWGwIIPldpVuNCCLQ{WwQVAvODR3IN88US=> M2nsR|I1PDV4NEey
SJSA1 cells NVL6eoQ3S3m2b4TvfIlkyqCjc4PhfS=> M4fSN|E3KGh? NHHvZoREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUlODMTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiBzNjDodpMh[nliRXTVJIlv[2:{cH;yZZRqd25iYYPzZZkhcW5icILld4Vv[2Vib3[gNVAmKGi3bXHuJJNmenWvLDDJR|UxRTBwMES1JO69VQ>? NGjmT2UzPDZyMU[0OC=>
RKO cells NXHmOpl[S3m2b4TvfIlkyqCjc4PhfS=> NH;iUYREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTU09iY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGVicEWzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1yLkC3JO69VQ>? NYjkRZBuOjN6MEi1OFU>
MDA-MB-435 cells MUjDfZRwfG:6aXRCpIF{e2G7 M4SyV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOg[ZhxemW|c3nu[{BxPTNibYX0ZY51KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHL5JG1VXCCjc4PhfUwhUUN3ME25MlEh|ryP NYS0UIh6OjN6MEi1OFU>
SW480 cells MW\DfZRwfG:6aXRCpIF{e2G7 NXrtVG5RS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW1d2OECgZ4VtdHNiZYjwdoV{e2mwZzDwOVMhdXW2YX70JIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGK7IF3UWEBie3OjeTygTWM2OD1zMz6zJO69VQ>? M4HKdVI{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

* 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
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02828930 Recruiting Solid Tumors Hoffmann-La Roche August 2016 Phase 1
NCT02670044 Recruiting Leukemia, Myeloid, Acute Hoffmann-La Roche March 2016 Phase 1|Phase 2
NCT02633059 Recruiting Recurrent Plasma Cell Myeloma Mayo Clinic|National Cancer Institute (NCI) December 2015 Phase 1|Phase 2
NCT02545283 Recruiting Neoplasms, Leukemia, Acute Myeloid Leukemia Hoffmann-La Roche December 2015 Phase 3
NCT02624986 Recruiting Non-Hodgkins Lymphoma Hoffmann-La Roche December 2015 Phase 1
NCT02407080 Recruiting Polycythemia Vera|Essential Thrombocythemia John Mascarenhas|Roche Pharma AG|The Leukemia and Lymphoma Society|Icahn School of Medicine at Mount Sinai April 2015 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.

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Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID