Drug Information

Drug (ID: DG01526) and It's Reported Resistant Information

• Name: FR900359
• Synonyms: FR900359; [(1R)-1-[(3S,6S,9S,12S,18R,21S,22R)-21-acetamido-18-benzyl-3-[(1R)-1-methoxyethyl]-4,9,10,12,16-pentamethyl-15-methylidene-2,5,8,11,14,17,20-heptaoxo-22-propan-2-yl-1,19-dioxa-4,7,10,13,16-pentazacyclodocos-6-yl]-2-methylpropyl] (2S,3R)-3-hydroxy-4-methyl-2-(propanoylamino)pentanoate; 107530-18-7; CHEMBL4171381; UBO-QIC; FR-900359; GTPL9336; SCHEMBL22133450; CHEBI:178012; BDBM50514449
• Target: .; NOUNIPROTAC; [1]
• Formula: 15
• IsoSMILES: CCC(=O)N[C@@H]([C@@H](C(C)C)O)C(=O)O[C@@H]([C@H]1C(=O)N([C@H](C(=O)O[C@@H]([C@@H](C(=O)O[C@@H](C(=O)N(C(=C)C(=O)N[C@H](C(=O)N([C@H](C(=O)N1)C)C)C)C)CC2=CC=CC=C2)NC(=O)C)C(C)C)[C@@H](C)OC)C)C(C)C
• InChI: InChI=1S/C49H75N7O15/c1-17-34(58)52-35(39(59)24(2)3)47(65)70-40(25(4)5)36-46(64)56(15)38(30(11)68-16)49(67)71-41(26(6)7)37(51-31(12)57)48(66)69-33(23-32-21-19-18-20-22-32)45(63)55(14)28(9)42(60)50-27(8)44(62)54(13)29(10)43(61)53-36/h18-22,24-27,29-30,33,35-41,59H,9,17,23H2,1-8,10-16H3,(H,50,60)(H,51,57)(H,52,58)(H,53,61)/t27-,29-,30+,33+,35-,36-,37-,38-,39+,40+,41+/m0/s1
• InChIKey: IMXKHFILKMPFGB-ZWYWTTNJSA-N
• PubChem CID: 14101198

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

  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

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Guanine nucleotide-binding protein subunit alpha-11 (GNA11) [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: UM002B cells; Brain; Homo sapiens (Human); N.A.
• In Vitro Model: Omm13 cells; N.A.; .; N.A.
• In Vitro Model: Ocm3 cells; Skin; Homo sapiens (Human); CVCL_6937
• In Vitro Model: 92-1 cells; Bladder; Homo sapiens (Human); CVCL_W909
• Experiment for Molecule Alteration: Sanger sequencing assay; Western blotting analysis

Unusual Activation of Pro-survival Pathway (UAPP)

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: UM002B cells; Brain; Homo sapiens (Human); N.A.
• In Vitro Model: Omm13 cells; N.A.; .; N.A.
• In Vitro Model: Ocm3 cells; Skin; Homo sapiens (Human); CVCL_6937
• In Vitro Model: 92-1 cells; Bladder; Homo sapiens (Human); CVCL_W909
• Experiment for Molecule Alteration: Sanger sequencing assay; Western blotting analysis

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: UM002B cells; Brain; Homo sapiens (Human); N.A.
• In Vitro Model: Omm13 cells; N.A.; .; N.A.
• In Vitro Model: Ocm3 cells; Skin; Homo sapiens (Human); CVCL_6937
• In Vitro Model: 92-1 cells; Bladder; Homo sapiens (Human); CVCL_W909
• Experiment for Molecule Alteration: Sanger sequencing assay; Western blotting analysis

References

• Ref 1: Effects of Oncogenic GAlpha(q) and GAlpha(11) Inhibition by FR900359 in Uveal MelanomaMol Cancer Res. 2019 Apr;17(4):963-973. doi: 10.1158/1541-7786.MCR-18-0574. Epub 2018 Dec 19.