Drug Information

Drug (ID: DG00326) and It's Reported Resistant Information

Name	Nutlin-3
Synonyms	Nutlin-3; 548472-68-0; 890090-75-2; nutlin-3A; nutlin 3; (+/-)-Nutlin3; CHEMBL211045; Nutlin 3(Random Configuration); MDM2 Antagonist, Nutlin-3, Racemic; 4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one; 4-({4,5-bis(4-chlorophenyl)-2-[4-methoxy-2-(propan-2-yloxy)phenyl]-4,5-dihydro-1H-imidazol-1-yl}carbonyl)piperazin-2-one; 4-[4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one Click to Show/Hide
Indication	In total 1 Indication(s) Discovery agent [ICD-11: N.A.] Investigative [1]
Structure
Drug Resistance Disease(s)	Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases) Prostate cancer [ICD-11: 2C82] [1]
Target	Cellular tumor antigen p53 (TP53)	P53_HUMAN	[1]
Target	Mdm2 messenger RNA (MDM2 mRNA)	MDM2_HUMAN	[1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula	C30H30Cl2N4O4
IsoSMILES	CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
InChI	1S/C30H30Cl2N4O4/c1-18(2)40-25-16-23(39-3)12-13-24(25)29-34-27(19-4-8-21(31)9-5-19)28(20-6-10-22(32)11-7-20)36(29)30(38)35-15-14-33-26(37)17-35/h4-13,16,18,27-28H,14-15,17H2,1-3H3,(H,33,37)
InChIKey	BDUHCSBCVGXTJM-UHFFFAOYSA-N
PubChem CID	216345
ChEBI ID	CHEBI:93777
TTD Drug ID	D01QKK

Type(s) of Resistant Mechanism of This Drug

EADR: Epigenetic Alteration of DNA, RNA or Protein

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Click to Show/Hide the Resistance Disease of This Class

Prostate cancer [ICD-11: 2C82]

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Drug Resistance Data Categorized by Their Corresponding Mechanisms
Epigenetic Alteration of DNA, RNA or Protein (EADR)			Click to Show/Hide
Key Molecule: Growth arrest specific 5 (GAS5)				[1]
Molecule Alteration	Expression		Down-regulation	Molecule Info
Resistant Disease	Prostate cancer [ICD-11: 2C82.0]			Disease Info
Experimental Note	Revealed Based on the Cell Line Data
Cell Pathway Regulation	Cell apoptosis		Inhibition	hsa04210
In Vitro Model	PC3 cells	Prostate	Homo sapiens (Human)	CVCL_0035
	22RV1 cells	Prostate	Homo sapiens (Human)	CVCL_1045
Experiment for Molecule Alteration	RT-PCR
Experiment for Drug Resistance	Fluorescence microscopy test apoptosis assay
Mechanism Description	Transient expression of GAS5 enhances apoptosis and decreases the survival of 22Rv1 cells, forced variation of GAS5 gene expression can modulate cellular responses to various apoptotic stimuli, including a range of chemotherapeutic drugs.

References

Ref 1	Long non-coding RNA GAS5 regulates apoptosis in prostate cancer cell lines. Biochim Biophys Acta. 2013 Oct;1832(10):1613-23. doi: 10.1016/j.bbadis.2013.05.005. Epub 2013 May 12.