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PF-04691502

PF-04691502 Struktur
1013101-36-4
CAS-Nr.
1013101-36-4
Englisch Name:
PF-04691502
Synonyma:
CS-305;CS-2640;PF4691502;PF-04691502;PF 04691502; PF04691502;PF-04691502 ISO 9001:2015 REACH;PF-04691502, 98%, a potent and selective inhibitor of PI3K and mTOR kinases;2-Amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3;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-methoxy-3-pyridinyl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
CBNumber:
CB22589602
Summenformel:
C22H27N5O4
Molgewicht:
425.48
MOL-Datei:
1013101-36-4.mol

PF-04691502 Eigenschaften

Schmelzpunkt:
219-221°C
Siedepunkt:
682.5±65.0 °C(Predicted)
Dichte
1.36
storage temp. 
Refrigerator
L?slichkeit
Chloroform (Slightly, Heated, Sonicated), Methanol (Slightly, Sonicated)
Aggregatzustand
Solid
pka
14.39±0.10(Predicted)
Farbe
Pale Yellow to Light Green

Sicherheit

PF-04691502 Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften

Pale Yellow Solid

Verwenden

PF-04691502 is an ATP-competitive PI3K/mTOR inhibitor with IC50 of 32 nM and also inhibits Akt T308/S473 with IC50 of 7.5 nM/3.8 nM.

Enzyminhibitor

This ATP-competitive PI3K/mTOR dual inhibitor (FW = 325.49 g/mol; CAS 1013101-36-4; Solubility = 14 mg/mL DMSO, < 1 mg/ML H2O), also systematically named 2-amino-8-((1R,4R)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)- one, potently inhibits recombinant Class-I PI3Kα (Ki = 1.8 nM), PI3Kβ (Ki = 2.1 nM), PI3Kδ (Ki = 1.6 nM), PI3Kγ (Ki = 1.9 nM), and mTOR (Ki = 16 nM) in biochemical assays, with little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 also suppresses avian fibroblast transformation mediated by wild-type PI3K γ, δ, or mutant PI3Kα. In PIK3CA-mutant and PTEN-deleted cancer cell lines, PF- 04691502 reduces phosphorylation of AKT T308 (IC50 = 7.5–47 nM) and AKT S473 (IC50 = 3.8–20 nM) and inhibits cell proliferation (IC50 = 180– 310 nM). PF-04691502 also inhibite mTORC1 activity within cells, asmeasured by PI3K-independent, nutrient-stimulated assay (IC50 = 32 nM) and inhibited the activation of PI3K and mTOR downstream effectors, including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1, and S6RP. Shortterm exposure to PF-04691502 predominantly inhibits PI3K, whereas mTOR inhibition persists for 24 to 48 hours. PF-04691502 also induces cell cycle G1 arrest, concomitant with upregulation of p27 Kip1 and reduction of retinbalstoma protein, or Rb. At doses below the maximal tolerable dose, PD-0325901 potently inhibits tumor growth, when Kras and/or PI3K are drivers of tumor growth and progression.

PF-04691502 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


PF-04691502 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 146)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Capot Chemical Co.,Ltd.
+86-(0)57185586718 +86-13336195806
sales@capot.com China 29791 60
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29880 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 965 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873
sales@chemdad.com China 39894 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63687 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32161 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226
sales@hzclap.com CHINA 6312 58
ANHUI WITOP BIOTECH CO., LTD
+8615255079626
eric@witopchemical.com China 23541 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 22784 58

  • PF-04691502
  • 2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
  • 2-aMino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-Methoxypyridin-3-yl)-4-Methylpyrido[2,3-d]pyriMidin-7(8H)-one
  • PF-04691502 2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
  • 2-Amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3
  • PF4691502
  • PF-04691502, 98%, a potent and selective inhibitor of PI3K and mTOR kinases
  • CS-2640
  • CS-305
  • PF 04691502; PF04691502
  • Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-
  • 2-amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one
  • PF-04691502 ISO 9001:2015 REACH
  • 2-Amino-8-(rel-(1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
  • 1013101-36-4
  • Akt
  • mTOR
  • PI3K
  • Inhibitors
  • PI3K/Akt/mTOR
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