PF-04691502

ChemicalBook > CAS DataBase List > PF-04691502

Product Name: PF-04691502
CAS No.: 1013101-36-4
Chemical Name: PF-04691502
Synonyms: 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
Molecular Formula: C22H27N5O4
Formula Weight: 425.48
MOL File: 1013101-36-4.mol

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PF-04691502 Property

Melting point:: 219-221°C
Boiling point:: 682.5±65.0 °C(Predicted)
Density: 1.36
storage temp.: Refrigerator
solubility: Chloroform (Slightly, Heated, Sonicated), Methanol (Slightly, Sonicated)
form: Solid
pka: 14.39±0.10(Predicted)
color: Pale Yellow to Light Green

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: PZ0235
Product name: PF-04691502
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $118
Updated: 2024/03/01

Sigma-Aldrich

Product number: PZ0235
Product name: PF-04691502
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $462
Updated: 2024/03/01

Cayman Chemical

Product number: 15017
Product name: PF-04691502
Purity: ≥95%
Packaging: 5mg
Price: $89
Updated: 2024/03/01

Cayman Chemical

Product number: 15017
Product name: PF-04691502
Purity: ≥95%
Packaging: 10mg
Price: $142
Updated: 2024/03/01

Cayman Chemical

Product number: 15017
Product name: PF-04691502
Purity: ≥95%
Packaging: 50mg
Price: $578
Updated: 2024/03/01

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PF-04691502 Chemical Properties,Usage,Production

Chemical Properties

Pale Yellow Solid

Uses

PF-04691502 is an potent and selective inihibitor of PI3K and mTOR Kinases with antitumor activity. Potent PI3K/mTOR Dual Inhibitor.

Uses

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.

Biological Activity

pf-04691502 is a potent and selective dual pi3k/mtor (frap) inhibitor to phosphorylation of akt t308 (ic50 = 7.5 nm) and akt s473 (ic50 = 3.8 nm).[1]pi3ks are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer.the functions of pi3ks most relate to the ability of class i pi3k to activate protein kinase b (pkb, aka akt) as in the pi3k/akt/mtor pathway which is an intracellular signaling pathway directly related to cellular quiescence, proliferation, cancer, and longevity. there are many valuable anti-cancer drug treatment targets within this pathway. and also the p110δ and p110γ isoforms regulate different aspects of immune responses. [2]pf-04691502 is a potential medical drug that functions by inhibiting class i pi3k and mtor in the pi3k/akt/mtor pathway through fluorescence polarization kinase assay, cell,mice and other animal trials, and therefore, through inhibition, results in tumour suppression.[3,4] short-term exposure to pf-04691502 predominantly inhibits pi3k, whereas mtor inhibition persists for 24 to 48 hours. pf-04691502 induces cell cycle g(1) arrest, concomitant with upregulation of p27 kip1 and reduction of rb. [5] antitumor activity of pf-04691502 is observed in u87 (pten null), skov3 (pik3ca mutation), and gefitinib- and erlotinib-resistant non-small cell lung carcinoma xenografts. pf-04691502 inhibits tumor growth at 7 days by 72%. fdg-pet imaging revealed that pf-04691502 reduces glucose metabolism dramatically. tissue biomarkers of pi3k/mtor pathway activity, p-akt (s473), and p-rps6 (s240/244), are also dramatically inhibited following pf-04691502 treatment. [6]

Enzyme inhibitor

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.

References

1. yuan j."pf-04691502, a potent and selective oral inhibitor of pi3k and mtor kinases with antitumor activity". mol cancer ther, 2011, 10(11), 2189-2199.2. okkenhaug k. "signaling by the phosphoinositide 3-kinase family in immune cells.".annu. rev. immunol, 2013. 17 (2): 675–699.3. maira, sauveur-michel; stauffer, frédéric; schnell, christian; garcía-echeverría, carlos. "pi3k inhibitors for cancer treatment: where do we stand ". biochemical society transactions., 2009. 37 (pt 1): 265–72.4. kinross km. "in vivo activity of combined pi3k/mtor and mek inhibition in a krasg12d; pten deletion mouse model of ovarian cancer". mol cancer ther, 2011, 10(8), 1440-1449.5. yuan j, mol cancer ther, 2011, 10(11), 2189-21996. kinross km, mol cancer ther, 2011, 10(8), 1440-1449

PF-04691502 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from PF-04691502 manufacturers

Dideu Industries Group Limited

Product: PF-04691502 1013101-36-4
Price: US $1.10/g
Min. Order: 1g
Purity: 99.00%
Supply Ability: 100 Tons Min
Release date: 2021-09-27

Career Henan Chemical Co

Product: PF-04691502 1013101-36-4
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

1013101-36-4, PF-04691502Related Search:

PF 477736 PF-562271 PF 573228 PF-05212384 PF-4708671 PF-562271HCl USP/EP/BP PF-04554878 PF-05231023 PF 05175157 PF-4634817 Everolimus Bortezomib Trametinib AZD5363 PLX4032 PF-5190457 [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate PF-06882961

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

PF4691502

2-Amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3

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