PZ0235

PF-04691502

≥98% (HPLC)

• Synonym(s): 2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one, PF-4691502, PF04691502
• Empirical Formula (Hill Notation): C₂₂H₂₇N₅O₄
• CAS Number: 1013101-36-4
• Molecular Weight: 425.48
• UNSPSC Code: 12352200
• PubChem Substance ID: 329823786
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: , white to yellow to light brown
• solubility: DMSO: 2 mg/mL, clear (warmed)
• storage temp.: room temp
• SMILES string: CC1=C(C(N([C@H]2CC[C@H](OCCO)CC2)C3=O)=NC(N)=N1)C=C3C4=CN=C(OC)C=C4
• 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)/t15-,16-
• InChI key: XDLYKKIQACFMJG-WKILWMFISA-N
• Gene Information: human ... MTOR(2475) , PIK3CA(5290) , PIK3CB(5291) , PIK3CD(5293) , PIK3CG(5294) , PIK3R1(5295) , PIK3R2(5296) , PIK3R3(8503) , PIK3R5(23533)

Description

Biochem/physiol Actions

PF-04691502 is a potent dual mTOR/PI3K inhibitor with Ki values of 1.6, 1.8, 1.9, 2.1 and 16 nM for human PI 3-K δ, α, β, γ, and mTOR, respectively, with no significant inhibitory activity at more than 80 other protein kinases, including PI 3-K downstream kinases, and MAPK family members. PF-04691502 showed antitumor activity in several non-small cell lung carcer (NSCLC) xenografts and ovarian cancer cell lines. PF-04691502 is currently in clinical trials.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable