RG7388 - 98%, high purity , Tumour suppressor p53/oncoprotein Mdm2 inhibitor, CAS No.1229705-06-9, Tumour suppressor p53/oncoprotein Mdm2 inhibitor

  • ≥98%
Item Number
R125598
Grouped product items
SKUSizeAvailabilityPrice Qty
R125598-5mg
5mg
In stock
$68.90
R125598-10mg
10mg
In stock
$117.90
R125598-25mg
25mg
In stock
$265.90
R125598-100mg
100mg
In stock
$484.90

Potent MDM2 inhibitor; inhibits MDM2-p53 interaction

Basic Description

SynonymsTVTXCJFHQKSQQM-LJQIRTBHSA-N | EN300-26181975 | RO5503781 | BP-25380 | 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid. | CLADRIBINE [MI] | UNII-5M84PX7JN2 | 4-((2
Specifications & Purity≥98%
Biochemical and Physiological MechanismsPotent MDM2 inhibitor (IC50= 6 nM in binding assay, and 30 nM in cancer cell proliferation assay). Induces p53 stabilisation, cell cycle arrest and apoptosis in cancer cells expression wildtype p53. Displays inhibition of tumor growth in the SJSA1 tumor x
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Action TypeINHIBITOR
Mechanism of actionTumour suppressor p53/oncoprotein Mdm2 inhibitor
Product Description

Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM.

Product Properties

ALogP4.3

Associated Targets(Human)

MDM2 Tchem E3 ubiquitin-protein ligase Mdm2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MDM2 Tchem p53-binding protein Mdm-2 (4545 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RKO (1376 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SW480 (6023 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCT-116 (91556 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDA-MB-435 (38290 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsomes (16955 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDM4 Tchem Protein Mdm4 (729 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TP53 Tchem Tumour suppressor p53/oncoprotein Mdm2 (2075 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SJSA-1 (970 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MOLM-14 (399 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MOLM-13 (2241 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OCI-AML-5 (18 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsome (341 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 4-[[(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-carbonyl]amino]-3-methoxybenzoic acid
INCHI InChI=1S/C31H29Cl2F2N3O4/c1-30(2,3)14-24-31(15-36,19-10-9-17(32)13-21(19)34)25(18-6-5-7-20(33)26(18)35)27(38-24)28(39)37-22-11-8-16(29(40)41)12-23(22)42-4/h5-13,24-25,27,38H,14H2,1-4H3,(H,37,39)(H,40,41)/t24-,25-,27+,31-/m0/s1
InChi Key TVTXCJFHQKSQQM-LJQIRTBHSA-N
Canonical SMILES CC(C)(C)CC1C(C(C(N1)C(=O)NC2=C(C=C(C=C2)C(=O)O)OC)C3=C(C(=CC=C3)Cl)F)(C#N)C4=C(C=C(C=C4)Cl)F
Isomeric SMILES CC(C)(C)C[C@H]1[C@]([C@H]([C@@H](N1)C(=O)NC2=C(C=C(C=C2)C(=O)O)OC)C3=C(C(=CC=C3)Cl)F)(C#N)C4=C(C=C(C=C4)Cl)F
PubChem CID 53358942
Molecular Weight 616.48

Certificates

Certificate of Analysis(COA)

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4 results found

Lot NumberCertificate TypeDateItem
I2205357Certificate of AnalysisJun 20, 2024 R125598
I2205358Certificate of AnalysisJun 20, 2024 R125598
I2205359Certificate of AnalysisJun 20, 2024 R125598
I2205360Certificate of AnalysisJun 20, 2024 R125598

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 61.65, Max Conc. mM: 100;DMSO (Slightly), Methanol (Slightly)

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H302:Harmful if swallowed

Precautionary Statements

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P301+P317:IF SWALLOWED: Get medical help.

Related Documents

Citations of This Product

1. Kang Chen, Xiu Xin, Lipeng Qiu, Wenpan Li, Guannan Guan, Gang Li, Mingxi Qiao, Xiuli Zhao, Haiyang Hu, Dawei Chen.  (2019)  Co-delivery of p53 and MDM2 inhibitor RG7388 using a hydroxyl terminal PAMAM dendrimer derivative for synergistic cancer therapy.  Acta Biomaterialia,  100  (118).  [PMID:31568878]

References

1. Kang Chen, Xiu Xin, Lipeng Qiu, Wenpan Li, Guannan Guan, Gang Li, Mingxi Qiao, Xiuli Zhao, Haiyang Hu, Dawei Chen.  (2019)  Co-delivery of p53 and MDM2 inhibitor RG7388 using a hydroxyl terminal PAMAM dendrimer derivative for synergistic cancer therapy.  Acta Biomaterialia,  100  (118).  [PMID:31568878]

Solution Calculators