Drug Information

Drug (ID: DG01547) and It's Reported Resistant Information

• Name: PF-04691502
• Synonyms: PF-04691502; 1013101-36-4; PF 04691502; 2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one; PF04691502; UNII-4W39NS61KI; 4W39NS61KI; CHEMBL1234354; PF-4691502; 2-Amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one; 2-Amino-8-[trans-4-(2-Hydroxyethoxy)cyclohexyl]-6-(6-Methoxypyridin-3-Yl)-4-Methylpyrido[2,3-D]pyrimidin-7(8h)-One; 2-Amino-8-(cis-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one; 2-Amino-8-(cis-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one; 4tv3; MLS006010979; GTPL7936; SCHEMBL1381425; SCHEMBL1381431; SCHEMBL1984896; SCHEMBL10092210; SCHEMBL13976989; EX-A032; QCR-137; HMS3656B21; AOB87714; BCP02895; BDBM50380313; MFCD18782794; NSC760536; NSC800846; s2743; ZINC58660483; AKOS005266645; AKOS030257531; ZINC100015733; ZINC117704832; CCG-268947; CS-0919; DB11974; NSC-760536; NSC-800846; SB20066; NCGC00346659-01; NCGC00381752-02; NCGC00381752-06; AC-28429; AS-17042; HY-15177; SMR004702782; BCP0726000275; PF4691502; SW220185-1; X7464; US8633204, 286; J-000360; PF-04691502, >=98% (HPLC); Q27088316; 2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one; Pyrido(2,3-d)pyrimidin-7(8H)-one, 2-amino-8-(trans-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxy-3-pyridinyl)-4-methyl-; trans-2-Amino-8-((1R,4R)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
• Indication:
  In total 3 Indication(s)
  Basal cell carcinoma [ICD-11: 2C32]; Phase 2; [1]
  Basal cell nevus syndrome [ICD-11: 2C32]; Phase 2; [1]
  Chondrosarcoma [ICD-11: 2B50]; Phase 2; [1]
• Target: Hedgehog signaling pathway (HS pathway); NOUNIPROTAC; [1]
• Formula: 6
• IsoSMILES: CC1=C2C=C(C(=O)N(C2=NC(=N1)N)C3CCC(CC3)OCCO)C4=CN=C(C=C4)OC
• InChI: InChI=1S/C22H27N5O4/c1-13-17-11-18(14-3-8-19(30-2)24-12-14)21(29)27(20(17)26-22(23)25-13)15-4-6-16(7-5-15)31-10-9-28/h3,8,11-12,15-16,28H,4-7,9-10H2,1-2H3,(H2,23,25,26)
• InChIKey: XDLYKKIQACFMJG-UHFFFAOYSA-N
• PubChem CID: 25033539
• TTD Drug ID: D0GD4Q
• DrugBank ID: DB11974

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

Ovarian cancer [ICD-11: 2C73]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

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

• Molecule Alteration: Missense mutation; p.H1047R (c.3140A>G)
• Sensitive Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: 293-MSR cells; Fetal kidney; Homo sapiens (Human); CVCL_KS18
• In Vivo Model: Female nu/nu mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Caspase-Glo 3/7 assay
• Mechanism Description: The missense mutation p.H1047R (c.3140A>G) in gene PIK3CA cause the sensitivity of PF-04691502 by aberration of the drug's therapeutic target

References

• Ref 1: PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activityMol Cancer Ther. 2011 Nov;10(11):2189-99. doi: 10.1158/1535-7163.MCT-11-0185. Epub 2011 Jul 12.