Drug Information

Drug (ID: DG01605) and It's Reported Resistant Information

• Name: SR-9009
• Synonyms: SR9009; 1379686-30-2; SR-9009; SR 9009; ethyl 3-[[(4-chlorophenyl)methyl-[(5-nitrothiophen-2-yl)methyl]amino]methyl]pyrrolidine-1-carboxylate; Stenabolic (SR9009); CHEMBL1961796; 1-Pyrrolidinecarboxylic acid, 3-((((4-chlorophenyl)methyl)((5-nitro-2-thienyl)methyl)amino)methyl)-, ethyl ester; Stenabolic; 1-pyrrolidinecarboxylic acid, 3-[[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-, ethyl ester; REV-ERB Agonist II; GTPL8901; EX-A726; BCP16215; BDBM50366238; MFCD29472236; NSC810521; s8692; AKOS027470307; CCG-269102; CS-4669; DB14013; NSC-810521; SB19006; NCGC00384202-01; AC-30219; AS-55859; HY-16989; A886340; J-690150; Q15410184; ethyl 3-(4-chlorobenzyl)((5-nitrothiophen-2-yl)methylaminomethyl)pyrrolidine-1-carboxylate; N'-[(1E)-1-(5-Chloro-2-hydroxyphenyl)ethylidene]-3-(4-morpholinylsulfonyl)benzohydrazide; ethyl 3-[[(4-chlorophenyl)methyl-[(5-nitro-2-thienyl)methyl]amino]methyl]pyrrolidine-1-carboxylate; Ethyl 3-[[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-1-pyrrolidinecarboxylate
• Indication:
  In total 1 Indication(s)
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Preclinical; [1]
• Target: ALK tyrosine kinase receptor (ALK); ALK_HUMAN; [1]
• Formula: 8
• IsoSMILES: CCOC(=O)N1CCC(C1)CN(CC2=CC=C(C=C2)Cl)CC3=CC=C(S3)[N+](=O)[O-]
• InChI: InChI=1S/C20H24ClN3O4S/c1-2-28-20(25)23-10-9-16(13-23)12-22(11-15-3-5-17(21)6-4-15)14-18-7-8-19(29-18)24(26)27/h3-8,16H,2,9-14H2,1H3
• InChIKey: MMJJNHOIVCGAAP-UHFFFAOYSA-N
• PubChem CID: 57394020
• TTD Drug ID: D0O9PQ
• DrugBank ID: DB14013

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: GTPase Hras (HRAS) [1]

• Molecule Alteration: Missense mutation; p.G12V (c.35G>T)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: HCT116 cells; Colon; Homo sapiens (Human); CVCL_0291
• In Vitro Model: A375 cells; Skin; Homo sapiens (Human); CVCL_0132
• In Vitro Model: Sk-Mel28 cells; Skin; Homo sapiens (Human); CVCL_0526
• In Vitro Model: T47D cells; Breast; Homo sapiens (Human); CVCL_0553
• In Vitro Model: PANC-1 cells; Pancreas; Homo sapiens (Human); CVCL_0480
• In Vitro Model: Jurkat cells; Pleural effusion; Homo sapiens (Human); CVCL_0065
• In Vitro Model: MCF-7 cells; Breast; Homo sapiens (Human); CVCL_0031
• In Vitro Model: WI38 cells; Fetal lung; Homo sapiens (Human); CVCL_0579
• In Vitro Model: BJ-ELR cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: BJ cells; Peripheral blood; Homo sapiens (Human); CVCL_E483
• In Vitro Model: Becker cells; N.A.; Homo sapiens (Human); CVCL_1093
• In Vivo Model: NOD mouse PDX model; Mus musculus
• Experiment for Molecule Alteration: Immunofluorescence microscopy assay; qRT-PCR
• Mechanism Description: Pharmacological modulation of circadian regulators is an effective novel antitumor strategy, identifying the existence of a previously unknown class of anticancer agents with a wide therapeutic window. REV-ERB agonists are novel autophagy and de novo lipogenesis inhibitors with selective activity towards malignant and benign neoplasms.

References

• Ref 1: Pharmacological activation of REV-ERBs is lethal in cancer and oncogene-induced senescenceNature. 2018 Jan 18;553(7688):351-355. doi: 10.1038/nature25170. Epub 2018 Jan 10.