Drug Information

Drug (ID: DG01529) and It's Reported Resistant Information

• Name: Voxtalisib
• Synonyms: Voxtalisib; 934493-76-2; SAR245409; 2-amino-8-ethyl-4-methyl-6-(1h-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7(8h)-one; UNII-CVL1685GPH; CVL1685GPH; Voxtalisib (XL765, SAR245409); Voxtalisib [USAN:INN]; Voxtalisib (USAN/INN); Voxtalisib (XL-765); SCHEMBL189573; CHEMBL3545366; CHEBI:124914; BCP16243; EX-A4140; BDBM50519385; NSC791226; NSC800972; s7646; ZINC35308805; 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7-one; AKOS037515701; CCG-267162; CS-3163; DB12400; NSC-791226; NSC-800972; SAR 245409; SB16573; Pyrido(2,3-d)pyrimidin-7(8H)-one, 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-3-yl)-; NCGC00387875-03; NCGC00387875-04; AC-29029; AS-56112; HY-15900; QC-11818; J3.527.559B; D11727; A855661; Q27215232; 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone
• Indication:
  In total 1 Indication(s)
  Hepatitis C virus infection [ICD-11: 1E50-1E51]; Phase 2; [1]
• Target: Human immunodeficiency virus Protease (HIV PR); POL_HV1B1; [1]
• Formula: 2
• IsoSMILES: CCN1C2=NC(=NC(=C2C=C(C1=O)C3=CC=NN3)C)N
• InChI: InChI=1S/C13H14N6O/c1-3-19-11-8(7(2)16-13(14)17-11)6-9(12(19)20)10-4-5-15-18-10/h4-6H,3H2,1-2H3,(H,15,18)(H2,14,16,17)
• InChIKey: RGHYDLZMTYDBDT-UHFFFAOYSA-N
• PubChem CID: 16123056
• ChEBI ID: CHEBI:124914
• TTD Drug ID: D04MCY
• DrugBank ID: DB12400

Type(s) of Resistant Mechanism of This Drug

  RTDM: Regulation by the Disease Microenvironment

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Breast cancer [ICD-11: 2C60]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Regulation by the Disease Microenvironment (RTDM)

Key Molecule: PI3-kinase alpha (PIK3CA) [1]

• Molecule Alteration: Missense mutation; p.E545K (c.1633G>A)
• Sensitive Disease: Breast adenocarcinoma [ICD-11: 2C60.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• In Vitro Model: MDA-MB-468 cells; Breast; Homo sapiens (Human); CVCL_0419
• In Vitro Model: U87-MG cells; Brain; Homo sapiens (Human); CVCL_0022
• In Vitro Model: LS174T cells; Colon; Homo sapiens (Human); CVCL_1384
• In Vitro Model: MCF-7 cells; Breast; Homo sapiens (Human); CVCL_0031
• In Vitro Model: Ramos cells; Ascites; Homo sapiens (Human); CVCL_0597
• In Vitro Model: OVCAR-3 cells; Ascites; Homo sapiens (Human); CVCL_0465
• In Vivo Model: Athymic nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: ViaLight HS assay; Apo-ONE Homogeneous Caspase-3/7 assay; Soft agar assay

References

• Ref 1: Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathwayMol Cancer Ther. 2014 May;13(5):1078-91. doi: 10.1158/1535-7163.MCT-13-0709. Epub 2014 Mar 14.