Drug Information

Drug (ID: DG01478) and It's Reported Resistant Information

• Name: Enzastaurin
• Synonyms: Enzastaurin; 170364-57-5; Enzastaurin (LY317615); LY317615; 3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione; LY-317615; UNII-UC96G28EQF; 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione; UC96G28EQF; LY 317615; CHEMBL300138; DB102; DSSTox_CID_24029; DSSTox_RID_80101; DSSTox_GSID_44029; 3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)-piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione; C32H29N5O2; 3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione; 3-(1-methyl-1H-indol-3-yl)-4-{1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1H-indol-3-yl}-1H-pyrrole-2,5-dione; CAS-170364-57-5; 3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione; LE-0014; Enzastaurin [USAN:INN]; Enzastaurin,LY317615; Enzastaurin; LY317615; LY317615 - Enzastaurin; SCHEMBL678748; GTPL5693; DTXSID5044029; CHEBI:91368; AMY7827; BCPP000241; HMS3265M05; HMS3265M06; HMS3265N05; HMS3265N06; HMS3654A13; HMS3748E03; BCP02703; EX-A1055; WHO 8426; ZINC1494900; Tox21_113367; BDBM50128285; DB-102; MFCD11040980; NSC767124; NSC800096; s1055; AKOS015994764; Tox21_113367_1; AC-5900; BCP9000648; CCG-264797; CS-0132; DB06486; NSC-767124; NSC-800096; SB16481; NCGC00238452-01; NCGC00238452-02; NCGC00238452-03; NCGC00238452-11; HY-10342; DB-064781; FT-0667873; SW219797-1; W3715; EC-000.2315; 364E575; J-510442; Q5381479; BRD-K79404599-001-01-0; 1H-Pyrrole-2,5-dione, 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-; 3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-1H-pyrrole-2,5-; 3-(1-Methyl-1H-indol-3-yl)-4-[1-(1-pyridin-2-ylmethyl-piperidin-4-yl)-1H-indol-3-yl]-pyrrole-2,5-dione; 3-(1-methyl-1H-indol-3-yl)-4-{1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1H-indol-3-yl}-2,5-dihydro-1H-pyrrole-2,5-dione
• Indication:
  In total 1 Indication(s)
  Convulsion [ICD-11: 8A61-8A6Z]; Phase 3; [1]
• Target: Fungal 1,3-beta-glucan synthase (Fung GSC2); FKS2_YEAST; [1]
• Formula: 5
• IsoSMILES: CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)C6CCN(CC6)CC7=CC=CC=N7
• InChI: InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39)
• InChIKey: AXRCEOKUDYDWLF-UHFFFAOYSA-N
• PubChem CID: 176167
• ChEBI ID: CHEBI:91368
• TTD Drug ID: D0F9BY
• VARIDT ID: DR1898
• DrugBank ID: DB06486

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

Uveal melanoma [ICD-11: 2D0Y]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Guanine nucleotide-binding protein alpha-q (GNAQ) [1]

• Molecule Alteration: Missense mutation; p.Q209P (c.626A>C)
• Sensitive Disease: Uveal melanoma [ICD-11: 2D0Y.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: Ocm3 cells; Skin; Homo sapiens (Human); CVCL_6937
• In Vitro Model: Ocm1 cells; Hypodermis; Homo sapiens (Human); CVCL_6934
• In Vitro Model: Mum2C cells; Hypodermis; Homo sapiens (Human); CVCL_3448
• In Vitro Model: Mum2B cells; Uveal melanoma; Homo sapiens (Human); CVCL_3447
• In Vitro Model: M619 cells; Skin; Homo sapiens (Human); CVCL_8472
• In Vitro Model: C918 cells; Skin; Homo sapiens (Human); CVCL_8471
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: MTS assay
• Mechanism Description: The missense mutation p.Q209P (c.626A>C) in gene GNAQ cause the sensitivity of Enzastaurin by unusual activation of pro-survival pathway

Key Molecule: Guanine nucleotide-binding protein alpha-q (GNAQ) [1]

• Molecule Alteration: Missense mutation; p.Q209L (c.626A>T)
• Sensitive Disease: Uveal melanoma [ICD-11: 2D0Y.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: Ocm3 cells; Skin; Homo sapiens (Human); CVCL_6937
• In Vitro Model: Ocm1 cells; Hypodermis; Homo sapiens (Human); CVCL_6934
• In Vitro Model: Mum2C cells; Hypodermis; Homo sapiens (Human); CVCL_3448
• In Vitro Model: Mum2B cells; Uveal melanoma; Homo sapiens (Human); CVCL_3447
• In Vitro Model: M619 cells; Skin; Homo sapiens (Human); CVCL_8472
• In Vitro Model: C918 cells; Skin; Homo sapiens (Human); CVCL_8471
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: MTS assay
• Mechanism Description: The missense mutation p.Q209L (c.626A>T) in gene GNAQ cause the sensitivity of Enzastaurin by unusual activation of pro-survival pathway

References

• Ref 1: The protein kinase C inhibitor enzastaurin exhibits antitumor activity against uveal melanomaPLoS One. 2012;7(1):e29622. doi: 10.1371/journal.pone.0029622. Epub 2012 Jan 12.