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PF-04691502 CAS: 1013101-36-4

Category: Inhibitors
Product Name: PF-04691502
Cat No: I000123
CAS No: 1013101-36-4
Synonyms: 2-amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one
Molecular Formula: C22H27N5O4
Molecular Weight: 425.5
SMILES: O=C1N([C@H]2CC[C@H](OCCO)CC2)C3=NC(N)=NC(C)=C3C=C1C4=CN=C(OC)C=C4
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)/t15-,16-
InChIKey: XDLYKKIQACFMJG-WKILWMFISA-N
Solubility: DMSO > 60 mg/mL Ethanol > 60 mg/mL
Target: PI3K
IC50: 1.8 nM/2.1 nM/1.6 nM/1.9 nM(PI3Kα/β/δ/γ); 16 nM(mTOR)
Storage: powder
CAS 1013101-36-4,PF-04691502
  • Description

PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.
IC50 value: 1.8 nM/2.1 nM/1.6 nM/1.9 nM(PI3Kα/β/δ/γ); 16 nM(mTOR)
Target: PI3K/mTOR
PF-04691502 is an ATP-competitive PI3K/mTOR dual inhibitor with IC50 of 32 nM. PF-04691502 is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PF-04691502 inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. PF-04691502 is currently in Phase II clinical trials in patients with recurrent endometrial cancer and Breast Cancer. A Phase II clinical trials in patients with solid tumors has been completed.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:Enhanced Anticancer Activity of PF-04691502, a Dual PI3K/mTOR Inhibitor, in Combination With VEGF siRNA Against Non-small-cell Lung Cancer. Espana-Serrano L, Chougule MB.Mol Ther Nucleic Acids. 2016 Nov 15;5(11):e384. doi: 10.1038/mtna.2016.90. PMID: 27845769 Free PMC Article
2:Inhibition of autophagy enhances effects of PF-04691502 on apoptosis and DNA damage of lung cancer cells. Fei HR, Tian H, Zhou XL, Yang MF, Sun BL, Yang XY, Jiao P, Wang FZ.Int J Biochem Cell Biol. 2016 Sep;78:52-62. doi: 10.1016/j.biocel.2016.06.023. Epub 2016 Jul 1. PMID: 27378731
3:A randomized phase II non-comparative study of PF-04691502 and gedatolisib (PF-05212384) in patients with recurrent endometrial cancer. Del Campo JM, Birrer M, Davis C, Fujiwara K, Gollerkeri A, Gore M, Houk B, Lau S, Poveda A, González-Martín A, Muller C, Muro K, Pierce K, Suzuki M, Vermette J, Oza A.Gynecol Oncol. 2016 Jul;142(1):62-9. doi: 10.1016/j.ygyno.2016.04.019. Epub 2016 Apr 24. PMID: 27103175
4:PF-04691502, a dual PI3K/mTOR inhibitor has potent pre-clinical activity by inducing apoptosis and G1 cell cycle arrest in aggressive B-cell non-Hodgkin lymphomas. Chen D, Mao C, Zhou Y, Su Y, Liu S, Qi WQ.Int J Oncol. 2016 Jan;48(1):253-60. doi: 10.3892/ijo.2015.3231. Epub 2015 Nov 5. PMID: 26549638
5:The PI3K/mTOR inhibitor PF-04691502 induces apoptosis and inhibits microenvironmental signaling in CLL and the Eµ-TCL1 mouse model. Blunt MD, Carter MJ, Larrayoz M, Smith LD, Aguilar-Hernandez M, Cox KL, Tipton T, Reynolds M, Murphy S, Lemm E, Dias S, Duncombe A, Strefford JC, Johnson PW, Forconi F, Stevenson FK, Packham G, Cragg MS, Steele AJ.Blood. 2015 Jun 25;125(26):4032-41. doi: 10.1182/blood-2014-11-610329. Epub 2015 May 8. PMID: 25957390 Free Article
6:Phase I study of PF-04691502, a small-molecule, oral, dual inhibitor of PI3K and mTOR, in patients with advanced cancer. Britten CD, Adjei AA, Millham R, Houk BE, Borzillo G, Pierce K, Wainberg ZA, LoRusso PM.Invest New Drugs. 2014 Jun;32(3):510-7. doi: 10.1007/s10637-013-0062-5. Epub 2014 Jan 7. Erratum in: Invest New Drugs. 2014 Jun;32(3):575. PMID: 24395457
7:Preclinical evaluation of the PI3K-mTOR dual inhibitor PF-04691502 as a novel therapeutic drug in nasopharyngeal carcinoma. Wong CH, Loong HH, Hui CW, Lau CP, Hui EP, Ma BB, Chan AT.Invest New Drugs. 2013 Dec;31(6):1399-408. doi: 10.1007/s10637-013-0007-z. Epub 2013 Aug 24. PMID: 23975511
8:Antitumor Efficacy of the Dual PI3K/mTOR Inhibitor PF-04691502 in a Human Xenograft Tumor Model Derived from Colorectal Cancer Stem Cells Harboring a PIK3CA Mutation. Fang DD, Zhang CC, Gu Y, Jani JP, Cao J, Tsaparikos K, Yuan J, Thiel M, Jackson-Fisher A, Zong Q, Lappin PB, Hayashi T, Schwab RB, Wong A, John-Baptiste A, Bagrodia S, Los G, Bender S, Christensen J, Vanarsdale T.PLoS One. 2013 Jun 27;8(6):e67258. doi: 10.1371/journal.pone.0067258. Print 2013. PMID: 23826249 Free PMC Article
9:PI3K/mTOR inhibitor PF-04691502 antitumor activity is enhanced with induction of wild-type TP53 in human xenograft and murine knockout models of head and neck cancer. Herzog A, Bian Y, Vander Broek R, Hall B, Coupar J, Cheng H, Sowers AL, Cook JD, Mitchell JB, Chen Z, Kulkarni AB, Van Waes C.Clin Cancer Res. 2013 Jul 15;19(14):3808-19. doi: 10.1158/1078-0432.CCR-12-2716. Epub 2013 May 2. PMID: 23640975 Free PMC Article
10:PF-04691502 triggers cell cycle arrest, apoptosis and inhibits the angiogenesis in hepatocellular carcinoma cells. Wang FZ, Peng-Jiao, Yang NN, Chuang-Yuan, Zhao YL, Liu QQ, Fei HR, Zhang JG.Toxicol Lett. 2013 Jul 4;220(2):150-6. doi: 10.1016/j.toxlet.2013.04.018. Epub 2013 Apr 29. PMID: 23639247


price inquiry for CAS:1013101-36-4, Product:PF-04691502