Drug Information

Drug (ID: DG01537) and It's Reported Resistant Information

• Name: Tirbanibulin
• Synonyms: KX2-391; 897016-82-9; Tirbanibulin; KX-01; N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide; UNII-4V9848RS5G; KX-2-391; KX-2391; CHEMBL571546; 4V9848RS5G; KX2391; KX2-391;KX-01; 2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]-~{N}-(phenylmethyl)ethanamide; Klisyri; KX 01; Tirbanibulin [USAN]; Tirbanibulin (USAN/INN); KX2-391 (Tirbanibulin); Tirbanibulin (KX2-391); MLS006011272; SCHEMBL153779; GTPL7957; KX01; DTXSID30237862; HMS3656J15; HMS3673E15; BCP02845; EX-A2434; XKB01682; BDBM50303801; NSC756643; NSC800779; s2700; WHO 10864; ZINC43152787; N-benzyl-2-(5-{4-[2-(morpholin-4-yl)ethoxy]phenyl}pyridin-2-yl)acetamide; N-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]acetamide; BCP9000828; CCG-264983; CS-0248; DB06137; KX2-391; KX-01; NSC-756643; NSC-800779; SB16619; 2-Pyridineacetamide, 5-(4-(2-(4-morpholinyl)ethoxy)phenyl)-n-(phenylmethyl)-; NCGC00346644-01; NCGC00346644-05; AS-73245; HY-10340; KX 2-391; SMR004703022; DB-119272; SW219670-1; X7515; C77028; D11691; A915990; BRD-K29968218-001-01-6; Q27888424; 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide; 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide; 2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]-N-(phenylmethyl)acetamide; 2-Pyridineacetamide,5-[4-[2-(4-morpholinyl)ethoxy]phenyl]-N-(phenylmethyl)-; 5-[4-[2-(4-Morpholinyl)ethoxy]phenyl]-N-(phenylmethyl)-2-pyridineacetamide; DN0
• Indication:
  In total 4 Indication(s)
  Breast cancer [ICD-11: 2C60]; Approved; [1]
  Breast cancer [ICD-11: 2C60]; Approved; [1]
  Non-hodgkin lymphoma [ICD-11: 2B33]; Approved; [1]
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Ovarian cancer [ICD-11: 2C73]; [1]
• Target: PI3-kinase gamma (PIK3CG); PK3CG_HUMAN; [1]
• Formula: 9
• IsoSMILES: C1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4
• InChI: InChI=1S/C26H29N3O3/c30-26(28-19-21-4-2-1-3-5-21)18-24-9-6-23(20-27-24)22-7-10-25(11-8-22)32-17-14-29-12-15-31-16-13-29/h1-11,20H,12-19H2,(H,28,30)
• InChIKey: HUNGUWOZPQBXGX-UHFFFAOYSA-N
• PubChem CID: 23635314
• TTD Drug ID: D08QGT
• DrugBank ID: DB06137

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

Ovarian cancer [ICD-11: 2C73]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Phosphatase and tensin homolog (PTEN) [1]

• Molecule Alteration: Missense mutation; p.G129R (c.385G>A)
• Resistant Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: RMUG-S; Ovary; Homo sapiens (Human); CVCL_3158
• In Vitro Model: RMUG-L; Endometrium; Homo sapiens (Human); CVCL_3157
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: MTT assay; EdU assay; Annexin V and 7-aminoactinomycin D assay; Flow cytometry analysis

References

• Ref 1: Targeting SRC and tubulin in mucinous ovarian carcinomaClin Cancer Res. 2013 Dec 1;19(23):6532-43. doi: 10.1158/1078-0432.CCR-13-1305. Epub 2013 Oct 7.