Drug Information

Drug (ID: DG01666) and It's Reported Resistant Information

• Name: XAV939
• Synonyms: XAV-939; 284028-89-3; XAV939; XAV 939; 3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one; 2-[4-(trifluoromethyl)phenyl]-1,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one; CHEBI:62878; C14H11F3N2OS; CHEMBL1086580; CID 2726824; 2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol; 2-[4-(trifluoromethyl)phenyl]-7,8-dihydro-5H-thiino[4,3-d]pyrimidin-4-ol; 2-[4-(Trifluoromethyl)phenyl]-7,8-Dihydro-5h-Thiopyrano[4,3-D]pyrimidin-4-Ol; NVP-XAV-939; 2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-3H-thiopyrano[4,3-d]pyrimidin-4(5H)-one; NVP-XAV 939; XAV; MFCD16879017; 3kr8; 3uh4; Maybridge3_005018; NVP-XAV939; MLS006012021; SCHEMBL7783488; TB3748-GMP; SCHEMBL15315468; AOB4150; DTXSID60369423; XAV939,XAV-939; BCPP000009; HMS1445E02; HMS3414D07; HMS3648B17; HMS3654O16; HMS3678D07; HMS3743E05; BCP02128; EX-A1760; BDBM50188594; BDBM50318567; NSC755761; s1180; ZINC13467799; AKOS015954858; AKOS024457786; AKOS026750243; CCG-208105; CS-0494; MCULE-6143908878; NSC-755761; SB19432; IDI1_016405; NCGC00250397-01; NCGC00484998-01; AC-28393; CS-10386; HY-15147; SMR003874205; XAV939, >=98% (HPLC); DB-067924; FT-0675873; SW218311-2; X7558; A25698; SR-01000946403; J-511234; SR-01000946403-1; BRD-K12762134-001-01-3; BRD-K12762134-001-05-4; Q27132250; 6,8-Dihydro-2-[4-(trifluoromethyl)phenyl]-5H-thiopyrano[3,4-d]pyrimidine; 2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-1H-thiopyrano[4,3-d]pyrimidin-4(5H)-one; 2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano-[4,3-d]pyrimidin-4-ol; 2-[4-(trifluoromethyl)phenyl]-1H,4H,5H,7H,8H-thiopyrano[4,3-d]pyrimidin-4-one
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Colorectal cancer [ICD-11: 2B91]; [1]
• Target: .; NOUNIPROTAC; [2]
• Formula: 1
• IsoSMILES: C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F
• InChI: InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)
• InChIKey: KLGQSVMIPOVQAX-UHFFFAOYSA-N
• PubChem CID: 135418940

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

Colorectal cancer [ICD-11: 2B91]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Adenomatous polyposis coli protein (APC) [1]

• Molecule Alteration: Nonsense; p.Q886* (c.2656C>T)
• Resistant Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Identified from the Human Clinical Data

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Adenomatous polyposis coli protein (APC) [2]

• Molecule Alteration: Nonsense; p.S811* (c.2432C>A)
• Sensitive Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Identified from the Human Clinical Data
• Cell Pathway Regulation: Wnt/Beta-catenin signaling pathway; Inhibition; hsa04310
• In Vitro Model: SW480 cells; Colon; Homo sapiens (Human); CVCL_0546
• In Vitro Model: RkO cells; Colon; Homo sapiens (Human); CVCL_0504
• In Vitro Model: HT-29 cells; Colon; Homo sapiens (Human); CVCL_0320
• In Vitro Model: SW403 cells; Colon; Homo sapiens (Human); CVCL_0545
• In Vitro Model: HCT-116 cells; Colon; Homo sapiens (Human); N.A.
• In Vitro Model: DLD-1 cells; Colon; Homo sapiens (Human); CVCL_0248
• In Vitro Model: HCT15 cells; Colon; Homo sapiens (Human); CVCL_0292
• In Vitro Model: KM-12 cells; Colon; Homo sapiens (Human); CVCL_1331
• In Vitro Model: HCC2998 cells; Colon; Homo sapiens (Human); CVCL_1266
• In Vitro Model: COLO-320DM cells; Colon; Homo sapiens (Human); CVCL_0219
• Experiment for Molecule Alteration: Immunofluorescence staining assay; Western blotting analysis
• Experiment for Drug Resistance: MTT assay

Key Molecule: Adenomatous polyposis coli protein (APC) [1]

• Molecule Alteration: Nonsense; p.Q1406* (c.4216C>T)
• Sensitive Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Identified from the Human Clinical Data

References

• Ref 1: Distinct Colorectal Cancer-Associated APC Mutations Dictate Response to Tankyrase InhibitionCancer Discov. 2019 Oct;9(10):1358-1371. doi: 10.1158/2159-8290.CD-19-0289. Epub 2019 Jul 23.
• Ref 2: APC Mutations as a Potential Biomarker for Sensitivity to Tankyrase Inhibitors in Colorectal CancerMol Cancer Ther. 2017 Apr;16(4):752-762. doi: 10.1158/1535-7163.MCT-16-0578. Epub 2017 Feb 8.