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Akt &GSK-3

PF-04691502 (1013101-36-4)

PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of1.8 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.

Not Intended for Therapeutic Use. For research use only.

CAS: 1013101-36-4 Category

PF-04691502 (1013101-36-4) Description

PF-04691502 is a PI3K/mTOR kinase inhibitor , 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.

PF-04691502 (1013101-36-4) Specifications

Product Name PF-04691502
Synonym PF04691502; PF 04691502; PF-04691502; PF4691502; PF 4691502; PF-4691502.
Chemical Name 2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
Purity ≥98% (HPLC)
CAS Number 1013101-36-4
Molecular Formula C22H27N5O4
Molecular Weight 425.48088
Monoisotopic Mass 425.2063 g/mol
MDL number N/A
InChIKey XDLYKKIQACFMJG-WKILWMFISA-N
InChi Code 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-
SMILES O=C1C(C2=CC=C(OC)N=C2)=CC3=C(C)N=C(N)N=C3N1[[email protected]]4CC[[email protected]](OCCO)CC4
Form Powder
Color White
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >5 years if stored properly
Handling Protect from air and moisture
Application PF-04691502 is a PI3K/mTOR kinase inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity [Erratum to document cited in CA155:552621] By Liu, Kevin K.-C.; Zhu, Jin Jiang; Smith, Graham L.; Yin, Min-Jean; Bailey, Simon; Chen, Jeffrey H.; Hu, Qiyue; Huang, Qinhua; Li, Chunze; Li, Qing J.; et al From ACS Medicinal Chemistry Letters, Ahead of Print.

[2].Treatment of cancers having k-ras mutations using PI3 kinase and HDAC inhibitors and preparation of bifunctional thienopyrimidine compounds that inhibit both enzymes By Bao, Rudi; Lai, Chengjung; Qian, Changgeng From PCT Int. Appl. (2011), WO 2011130628 A1 20111020.

[3]. Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity By Liu, Kevin K.-C.; Zhu, Jin Jiang; Smith, Graham L.; Yin, Min-Jean; Bailey, Simon; Chen, Jeffrey H.; Hu, Qiyue; Huang, Qinhua; Li, Chunze; Li, Qing J.; et al From ACS Medicinal Chemistry Letters (2011), 2(11), 809-813.

[4]. In vivo activity of combined PI3K/mTOR and MEK inhibition in a KrasG12D;Pten deletion mouse model of ovarian cancer By Kinross, Kathryn M.; Brown, Daniel V.; Kleinschmidt, Margarete; Jackson, Susan; Christensen, James; Cullinane, Carleen; Hicks, Rodney J.; Johnstone, Ricky W.; McArthur, Grant A. From Molecular Cancer Therapeutics (2011), 10(8), 1440-1449.

[5]. Detection of oncogenic mutations as markers of susceptibility of tumors to treatment with inhibitors of HSP90 and associated signaling proteins By Fritz, Christian; Normant, Emmanuel Y.; Paez, Juan Guillermo; West, Kip A. From PCT Int. Appl. (2011), WO 2011060328 A1 20110519.

1 review for PF-04691502 (1013101-36-4)

  1. Cofttek

    Never had such good experience before,The PF-04691502 (1013101-36-4) is high purity,also customer service is pretty nice !gotta try!!

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