Drug Information

Drug (ID: DG01481) and It's Reported Resistant Information

• Name: TASIN-1
• Synonyms: TASIN-1; 792927-06-1; 1'-((4-methoxyphenyl)sulfonyl)-4-methyl-1,4'-bipiperidine; 1-[1-(4-methoxyphenyl)sulfonylpiperidin-4-yl]-4-methylpiperidine; 1'-[(4-methoxyphenyl)sulfonyl]-4-methyl-1,4'-bipiperidine; CHEMBL4514756; SCHEMBL17007497; ZINC4744379; NSC766210; STK193520; AKOS003649063; HY-116572A; MCULE-6685404683; NSC-766210; AT-057/43468793; 1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine
• Target: .; NOUNIPROTAC; [1]
• Formula: 4
• IsoSMILES: CC1CCN(CC1)C2CCN(CC2)S(=O)(=O)C3=CC=C(C=C3)OC
• InChI: InChI=1S/C18H28N2O3S/c1-15-7-11-19(12-8-15)16-9-13-20(14-10-16)24(21,22)18-5-3-17(23-2)4-6-18/h3-6,15-16H,7-14H2,1-2H3
• InChIKey: XCBHYDPDIJQQGM-UHFFFAOYSA-N
• PubChem CID: 1329829

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

Colorectal cancer [ICD-11: 2B91]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Adenomatous polyposis coli protein (APC) [1]

• Molecule Alteration: Missense mutation; p.G1416* (c.4246_4248delGGCinsTGA)
• Sensitive Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HT29 Cells; Colon; Homo sapiens (Human); CVCL_A8EZ
• In Vitro Model: SW480 cells; Colon; Homo sapiens (Human); CVCL_0546
• In Vitro Model: DLD1 cells; Colon; Homo sapiens (Human); CVCL_0248
• In Vitro Model: SW620 cells; Colon; Homo sapiens (Human); CVCL_0547
• In Vitro Model: HCT116 cells; Colon; Homo sapiens (Human); CVCL_0291
• In Vitro Model: RkO cells; Colon; Homo sapiens (Human); CVCL_0504
• In Vitro Model: NCI-H508 cells; Colon; Homo sapiens (Human); CVCL_1564
• In Vitro Model: SW948 cells; Colon; Homo sapiens (Human); CVCL_0632
• In Vitro Model: HT55 cells; Colon; Homo sapiens (Human); CVCL_1294
• In Vitro Model: SW403 cells; Colon; Homo sapiens (Human); CVCL_0545
• In Vitro Model: 293FT cells; Kidney; Homo sapiens (Human); CVCL_6911
• In Vitro Model: T84 cells; Colon; Homo sapiens (Human); CVCL_0555
• In Vitro Model: HCEC cells; N.A.; .; N.A.
• In Vivo Model: Female athymic nude mouse PDX model; Mus musculus
• Experiment for Drug Resistance: Promega assay
• Mechanism Description: TASIN-1 exerts its cytotoxic effects through inhibition of cholesterol biosynthesis.

Key Molecule: Adenomatous polyposis coli protein (APC) [1]

• Molecule Alteration: Nonsense; p.E1309* (c.3925G>T)
• Sensitive Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HT29 Cells; Colon; Homo sapiens (Human); CVCL_A8EZ
• In Vitro Model: SW480 cells; Colon; Homo sapiens (Human); CVCL_0546
• In Vitro Model: DLD1 cells; Colon; Homo sapiens (Human); CVCL_0248
• In Vitro Model: SW620 cells; Colon; Homo sapiens (Human); CVCL_0547
• In Vitro Model: HCT116 cells; Colon; Homo sapiens (Human); CVCL_0291
• In Vitro Model: RkO cells; Colon; Homo sapiens (Human); CVCL_0504
• In Vitro Model: NCI-H508 cells; Colon; Homo sapiens (Human); CVCL_1564
• In Vitro Model: SW948 cells; Colon; Homo sapiens (Human); CVCL_0632
• In Vitro Model: HT55 cells; Colon; Homo sapiens (Human); CVCL_1294
• In Vitro Model: SW403 cells; Colon; Homo sapiens (Human); CVCL_0545
• In Vitro Model: 293FT cells; Kidney; Homo sapiens (Human); CVCL_6911
• In Vitro Model: T84 cells; Colon; Homo sapiens (Human); CVCL_0555
• In Vitro Model: HCEC cells; N.A.; .; N.A.
• In Vivo Model: Female athymic nude mouse PDX model; Mus musculus
• Experiment for Drug Resistance: Promega assay
• Mechanism Description: TASIN-1 exerts its cytotoxic effects through inhibition of cholesterol biosynthesis.

Key Molecule: Adenomatous polyposis coli protein (APC) [1]

• Molecule Alteration: Nonsense; p.Q1338* (c.4012C>T)
• Sensitive Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HT29 Cells; Colon; Homo sapiens (Human); CVCL_A8EZ
• In Vitro Model: SW480 cells; Colon; Homo sapiens (Human); CVCL_0546
• In Vitro Model: DLD1 cells; Colon; Homo sapiens (Human); CVCL_0248
• In Vitro Model: SW620 cells; Colon; Homo sapiens (Human); CVCL_0547
• In Vitro Model: HCT116 cells; Colon; Homo sapiens (Human); CVCL_0291
• In Vitro Model: RkO cells; Colon; Homo sapiens (Human); CVCL_0504
• In Vitro Model: NCI-H508 cells; Colon; Homo sapiens (Human); CVCL_1564
• In Vitro Model: SW948 cells; Colon; Homo sapiens (Human); CVCL_0632
• In Vitro Model: HT55 cells; Colon; Homo sapiens (Human); CVCL_1294
• In Vitro Model: SW403 cells; Colon; Homo sapiens (Human); CVCL_0545
• In Vitro Model: 293FT cells; Kidney; Homo sapiens (Human); CVCL_6911
• In Vitro Model: T84 cells; Colon; Homo sapiens (Human); CVCL_0555
• In Vitro Model: HCEC cells; N.A.; .; N.A.
• In Vivo Model: Female athymic nude mouse PDX model; Mus musculus
• Experiment for Drug Resistance: Promega assay
• Mechanism Description: TASIN-1 exerts its cytotoxic effects through inhibition of cholesterol biosynthesis.

References

• Ref 1: Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancerSci Transl Med. 2016 Oct 19;8(361):361ra140. doi: 10.1126/scitranslmed.aaf8127.