Drug Information

Drug (ID: DG01834) and It's Reported Resistant Information

• Name: Erastin
• Synonyms: ERASTIN; 571203-78-6; 2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-Quinazolinone; 2-(1-(4-(2-(4-chlorophenoxy)acetyl)piperazin-1-yl)ethyl)-3-(2-ethoxyphenyl)quinazolin-4(3H)-one; MFCD09837984; 2-[1-[4-[2-(4-chlorophenoxy)acetyl]piperazin-1-yl]ethyl]-3-(2-ethoxyphenyl)quinazolin-4-one; CHEMBL401989; SCHEMBL4457820; Erastin, >=98% (HPLC); CHEBI:94287; AOB6043; DTXSID80458949; EX-A295; HMS3653K21; HMS3868M03; BCP27907; WXA20378; 2400AH; BDBM50376126; s7242; AKOS025147365; CCG-269987; CS-1675; Erastin - CAS 571203-78-6; SB19588; NCGC00351608-10; NCGC00351608-14; AS-55898; DA-42059; HY-15763; QC-11375; FT-0700333; SW208651-2; C21478; A869751; BRD-A25004090-001-01-9; BRD-A25004090-001-02-7; BRD-A25004090-001-06-8; Q27166099; 2-[1-[4-[2-(4-chlorophenoxy)-1-oxoethyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4-quinazolinone; 4(3H)-Quinazolinone, 2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Liver cancer [ICD-11: 2C12]; [1]
• Target: Sigma intracellular receptor 2 (TMEM97); SGMR2_HUMAN; [1]
• Formula: 8
• IsoSMILES: CCOC1=CC=CC=C1N2C(=O)C3=CC=CC=C3N=C2C(C)N4CCN(CC4)C(=O)COC5=CC=C(C=C5)Cl
• InChI: InChI=1S/C30H31ClN4O4/c1-3-38-27-11-7-6-10-26(27)35-29(32-25-9-5-4-8-24(25)30(35)37)21(2)33-16-18-34(19-17-33)28(36)20-39-23-14-12-22(31)13-15-23/h4-15,21H,3,16-20H2,1-2H3
• InChIKey: BKQFRNYHFIQEKN-UHFFFAOYSA-N
• PubChem CID: 11214940
• ChEBI ID: CHEBI:94287

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Diffuse large B-cell lymphoma [ICD-11: 2A81]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: CDGSH iron-sulfur domain-containing protein 2 (CISD2) [2]

• Sensitive Disease: Diffuse large B-cell lymphoma [ICD-11: 2A81.0]
• Molecule Alteration: Expression; Down-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HBL-1/DOX cells; Lymph; Homo sapiens (Human); N.A.
• Experiment for Drug Resistance: CCK8 assay; Cell proliferation assay
• Mechanism Description: A decrease in cell proliferation was observed in HBL-1/DOX cells transfected with shCISD2 and treated with 10 µM Erastin, compared to the inhibition of shCISD2 in HBL-1/DOX cells . Additionally, increases in iron , MDA , and ROS generation were induced by Erastin , while decreases in GSH and MMPs were also observed. Treatment of HBL-1/DOX cells with a combination of Erastin and shCISD2 resulted in a decrease in CISD2, p62, FTH1, and GPX4 levels, along with an increase in BECN1 and NCOA4. These findings suggest that inhibiting CISD2 can enhance the effects of Erastin by promoting increased ferroptosis and ferritinophagy, thereby contributing to the cell death of HBL-1/DOX cells.

Esophageal cancer [ICD-11: 2B70]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Acidic leucine-rich nuclear phosphoprotein 32 family member E (ANP32E) [3]

• Sensitive Disease: Oesophagus adenocarcinoma [ICD-11: 2B70.0]
• Molecule Alteration: Expression; Down-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Ferroptosis signaling pathway; Activation; hsa04216
• In Vitro Model: KYSE150 cells; Esophagus; Homo sapiens (Human); CVCL_1348
• In Vitro Model: KYSE-30 cells; Esophagus; Homo sapiens (Human); CVCL_1351
• Experiment for Molecule Alteration: Western blot assay
• Experiment for Drug Resistance: CCK8 assay; Colony formation assay
• Mechanism Description: Repression of ANP32E increases the responsiveness of EC to PTX, and the concurrent use of erastin with PTX enhances their anti-cancer effectiveness. These findings provide support for the efficacy of inducing ferroptosis as a potential therapeutic approach to enhance the cytotoxic effects of PTX. ANP32E regulates EC progression and ferroptosis through the p53/SLC7A11 axis, offering a potential molecular target for overcoming PTX resistance in EC treatment.

Liver cancer [ICD-11: 2C12]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: GABPB1 antisense RNA 1 (GABPB1-AS1) [1]

• Resistant Disease: Cholangiocarcinoma [ICD-11: 2C12.0]
• Molecule Alteration: Down-regulation; Interaction
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: HepG2 cells; Liver; Homo sapiens (Human); CVCL_0027
• In Vitro Model: Hep3B cells; Liver; Homo sapiens (Human); CVCL_0326
• In Vitro Model: Huh7 cells; Kidney; Homo sapiens (Human); CVCL_U442
• Experiment for Drug Resistance: CCK8 assay
• Mechanism Description: LncRNA GABPB1-AS1 and GABPB1 regulate oxidative stress during erastin-induced ferroptosis in HepG2 hepatocellular carcinoma cells.

References

• Ref 1: LncRNA GABPB1-AS1 and GABPB1 regulate oxidative stress during erastin-induced ferroptosis in HepG2 hepatocellular carcinoma cellsSci Rep. 2019 Nov 7;9(1):16185. doi: 10.1038/s41598-019-52837-8.
• Ref 2: Inhibition of CISD2 enhances sensitivity to doxorubicin in diffuse large B-cell lymphoma by regulating ferroptosis and ferritinophagy. Front Pharmacol. 2024 Nov 13;15:1482354.
• Ref 3: ANP32E promotes esophageal cancer progression and paclitaxel resistance via P53/SLC7A11 axis-regulated ferroptosis. Int Immunopharmacol. 2025 Jan 10;144:113436.