Drug Information

Drug (ID: DG01512) and It's Reported Resistant Information

• Name: Spliceostatin A
• Synonyms: Spliceostatin A; [(Z,2S)-4-[[(2R,3R,5S,6S)-6-[(2E,4E)-5-[(3R,4R,5R,7S)-4-hydroxy-7-methoxy-7-methyl-1,6-dioxaspiro[2.5]octan-5-yl]-3-methylpenta-2,4-dienyl]-2,5-dimethyloxan-3-yl]carbamoyl]but-3-en-2-yl] acetate; 391611-36-2; CHEMBL1221942; SCHEMBL18134895; BP-28004; Q59780090; (2Z,4S)-N-[(2R,3R,5S,6S)-2,5-Dimethyl-6-[(2E)-3-methyl-5-[(3R,4R,5R,7S)-4-hydroxy-7-methoxy-7-methyl-1,6-dioxaspiro[2.5]octane-5-yl]-2,4-pentadienyl]tetrahydro-2H-pyran-3-yl]-4-acetoxy-2-penteneamide
• Target: .; NOUNIPROTAC; [1]
• Formula: 10
• IsoSMILES: C[C@H]1C[C@H]([C@H](O[C@H]1C/C=C(\\C)/C=C/[C@@H]2[C@H]([C@@]3(C[C@@](O2)(C)OC)CO3)O)C)NC(=O)/C=C\\[C@H](C)OC(=O)C
• InChI: InChI=1S/C28H43NO8/c1-17(9-12-24-26(32)28(16-34-28)15-27(6,33-7)37-24)8-11-23-18(2)14-22(20(4)36-23)29-25(31)13-10-19(3)35-21(5)30/h8-10,12-13,18-20,22-24,26,32H,11,14-16H2,1-7H3,(H,29,31)/b12-9+,13-10-,17-8+/t18-,19-,20+,22+,23-,24+,26+,27-,28+/m0/s1
• InChIKey: XKSGIJNRMWHQIQ-CGPJBNNXSA-N
• PubChem CID: 10673568

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Pancreatic cancer [ICD-11: 2C10]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Splicing factor 3B subunit 1 (SF3B1) [1]

• Molecule Alteration: Missense mutation; p.K700E (c.2098A>G)
• Sensitive Disease: Pancreatic ductal adenocarcinoma [ICD-11: 2C10.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: PANC-1 cells; Pancreas; Homo sapiens (Human); CVCL_0480
• In Vitro Model: Capan-1 cells; Pancreas; Homo sapiens (Human); CVCL_0237
• In Vitro Model: Capan-2 cells; Pancreas; Homo sapiens (Human); CVCL_0026
• In Vitro Model: HEC1A cells; Uterus; Homo sapiens (Human); CVCL_0293
• In Vitro Model: Capan-1 cells; Pancreas; Homo sapiens (Human); CVCL_0237
• In Vitro Model: Capan-2 cells; Pancreas; Homo sapiens (Human); CVCL_0026
• In Vitro Model: Pancreatic Panc 0504 cells; Pancreas; Homo sapiens (Human); CVCL_1637
• In Vitro Model: MFE296 cells; Endometrium; Homo sapiens (Human); CVCL_1406
• In Vitro Model: HEC59 cells; Endometrium; Homo sapiens (Human); CVCL_2930
• In Vitro Model: ESS-1 cells; Endometrium; Homo sapiens (Human); CVCL_1205
• In Vitro Model: DSMZ cells; N.A.; .; N.A.
• In Vitro Model: ESS-1 cells; Endometrium; Homo sapiens (Human); CVCL_1205
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: CellTiter-Glo assay

Breast cancer [ICD-11: 2C60]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Splicing factor 3B subunit 1 (SF3B1) [1]

• Molecule Alteration: Missense mutation; p.K666N (c.1998G>T)
• Sensitive Disease: Breast adenocarcinoma [ICD-11: 2C60.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: PANC-1 cells; Pancreas; Homo sapiens (Human); CVCL_0480
• In Vitro Model: Capan-1 cells; Pancreas; Homo sapiens (Human); CVCL_0237
• In Vitro Model: Capan-2 cells; Pancreas; Homo sapiens (Human); CVCL_0026
• In Vitro Model: HEC1A cells; Uterus; Homo sapiens (Human); CVCL_0293
• In Vitro Model: Capan-1 cells; Pancreas; Homo sapiens (Human); CVCL_0237
• In Vitro Model: Capan-2 cells; Pancreas; Homo sapiens (Human); CVCL_0026
• In Vitro Model: Pancreatic Panc 0504 cells; Pancreas; Homo sapiens (Human); CVCL_1637
• In Vitro Model: MFE296 cells; Endometrium; Homo sapiens (Human); CVCL_1406
• In Vitro Model: HEC59 cells; Endometrium; Homo sapiens (Human); CVCL_2930
• In Vitro Model: ESS-1 cells; Endometrium; Homo sapiens (Human); CVCL_1205
• In Vitro Model: DSMZ cells; N.A.; .; N.A.
• In Vitro Model: ESS-1 cells; Endometrium; Homo sapiens (Human); CVCL_1205
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: CellTiter-Glo assay

Key Molecule: Splicing factor 3B subunit 1 (SF3B1) [1]

• Molecule Alteration: Missense mutation; p.K700E (c.2098A>G)
• Sensitive Disease: Breast adenocarcinoma [ICD-11: 2C60.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: PANC-1 cells; Pancreas; Homo sapiens (Human); CVCL_0480
• In Vitro Model: Capan-1 cells; Pancreas; Homo sapiens (Human); CVCL_0237
• In Vitro Model: Capan-2 cells; Pancreas; Homo sapiens (Human); CVCL_0026
• In Vitro Model: HEC1A cells; Uterus; Homo sapiens (Human); CVCL_0293
• In Vitro Model: Capan-1 cells; Pancreas; Homo sapiens (Human); CVCL_0237
• In Vitro Model: Capan-2 cells; Pancreas; Homo sapiens (Human); CVCL_0026
• In Vitro Model: Pancreatic Panc 0504 cells; Pancreas; Homo sapiens (Human); CVCL_1637
• In Vitro Model: MFE296 cells; Endometrium; Homo sapiens (Human); CVCL_1406
• In Vitro Model: HEC59 cells; Endometrium; Homo sapiens (Human); CVCL_2930
• In Vitro Model: ESS-1 cells; Endometrium; Homo sapiens (Human); CVCL_1205
• In Vitro Model: DSMZ cells; N.A.; .; N.A.
• In Vitro Model: ESS-1 cells; Endometrium; Homo sapiens (Human); CVCL_1205
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: CellTiter-Glo assay

Endometrial cancer [ICD-11: 2C76]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Splicing factor 3B subunit 1 (SF3B1) [1]

• Molecule Alteration: Missense mutation; p.K666N (c.1998G>C)
• Sensitive Disease: Endometrial adenocarcinoma [ICD-11: 2C76.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: PANC-1 cells; Pancreas; Homo sapiens (Human); CVCL_0480
• In Vitro Model: Capan-1 cells; Pancreas; Homo sapiens (Human); CVCL_0237
• In Vitro Model: Capan-2 cells; Pancreas; Homo sapiens (Human); CVCL_0026
• In Vitro Model: HEC1A cells; Uterus; Homo sapiens (Human); CVCL_0293
• In Vitro Model: Capan-1 cells; Pancreas; Homo sapiens (Human); CVCL_0237
• In Vitro Model: Capan-2 cells; Pancreas; Homo sapiens (Human); CVCL_0026
• In Vitro Model: Pancreatic Panc 0504 cells; Pancreas; Homo sapiens (Human); CVCL_1637
• In Vitro Model: MFE296 cells; Endometrium; Homo sapiens (Human); CVCL_1406
• In Vitro Model: HEC59 cells; Endometrium; Homo sapiens (Human); CVCL_2930
• In Vitro Model: ESS-1 cells; Endometrium; Homo sapiens (Human); CVCL_1205
• In Vitro Model: DSMZ cells; N.A.; .; N.A.
• In Vitro Model: ESS-1 cells; Endometrium; Homo sapiens (Human); CVCL_1205
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: CellTiter-Glo assay

References

• Ref 1: SF3B1 mutations constitute a novel therapeutic target in breast cancerJ Pathol. 2015 Mar;235(4):571-80. doi: 10.1002/path.4483. Epub 2014 Dec 22.