2-アミノ-4-メチル-6-(6-メトキシピリジン-3-イル)-8-[4β-(2-ヒドロキシエチルオキシ)シクロヘキサン-1α-イル]ピリド[2,3-d]ピリミジン-7(8H)-オン

2-アミノ-4-メチル-6-(6-メトキシピリジン-3-イル)-8-[4β-(2-ヒドロキシエチルオキシ)シクロヘキサン-1α-イル]ピリド[2,3-d]ピリミジン-7(8H)-オン 価格

2-アミノ-4-メチル-6-(6-メトキシピリジン-3-イル)-8-[4β-(2-ヒドロキシエチルオキシ)シクロヘキサン-1α-イル]ピリド[2,3-d]ピリミジン-7(8H)-オン 化学特性,用途語,生産方法

• 用途

  PI3-K/mTOR に対するデュアル阻害剤です。ATP 競合性です

• 用途

  PI3-K/mTOR に対するデュアル阻害剤です。ATP 競合性です。

• 化学的特性

  Pale Yellow Solid

• 使用

  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.

• 酵素阻害剤

  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.

2-アミノ-4-メチル-6-(6-メトキシピリジン-3-イル)-8-[4β-(2-ヒドロキシエチルオキシ)シクロヘキサン-1α-イル]ピリド[2,3-d]ピリミジン-7(8H)-オン 生産企業

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2-アミノ-4-メチル-6-(6-メトキシピリジン-3-イル)-8-[4β-(2-ヒドロキシエチルオキシ)シクロヘキサン-1α-イル]ピリド[2,3-d]ピリミジン-7(8H)-オン スペクトルデータ(¹HNMR)

1013101-36-4, 2-アミノ-4-メチル-6-(6-メトキシピリジン-3-イル)-8-[4β-(2-ヒドロキシエチルオキシ)シクロヘキサン-1α-イル]ピリド[2,3-d]ピリミジン-7(8H)-オン キーワード