PHA-665752

PHA-665752 価格

PHA-665752 化学特性,用途語,生産方法

• 溶解性

  In vitro (25℃) DMSO 128 mg/mL (199.49 mM)

• 用途

  強 力 で 選択的 な MET キ ナ ー ゼ 阻 害 剤（IC50 = 9 nmol/l（MET），68 nmol/l（Ron），200 nmol/l（Flk-1），1,400 nmol/l（c-abl），3,000 nmol/l（FGFR1），3,800 nmol/l（EGFR），6,000 nmol/l（c-src）。ATP 競合性です。抗がん作用を示します。

• 用途

  強力で選択的な MET キナーゼ阻害剤（IC50 = 9 nM（MET），68 nM（Ron），200 nM（Flk-1）， 1,400 nM（c-abl），3,000 nM（FGFR1），3,800 nM（EGFR），6,000 nM（c-src）。ATP 競合 性です。抗がん作用を示します。

• 説明

  The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers. PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (K_i = 4 nM; IC₅₀ = 9 nM). It exhibits >50-fold selectivity for c-Met over a panel of tyrosine and serine/threonine kinases. PHA-665752 can inhibit c-Met phosphorylation, as well as cell proliferation and cell motility, of various tumor cells (IC₅₀s = 18-50 nM). It also inhibits signal transduction downstream of c-Met, interfering with the activation of Gab-1 adaptor protein, ERK1/2, Akt, STAT3, PLC-γ, and focal adhesion kinase in multiple tumor cell lines. In a gastric carcinoma xenograft model, 25 mg/kg PHA-665752 was shown to reduce tumor growth in mice by inhibiting c-Met activation.

• 化学的特性

  Yellow powder crystal

• 使用

  PHA-665752 ia a c-Met kinase inhibitor. PHA-665752 is ATP-competitive, an active-site inhibitor with greater than 50-fold selectivity for c-Met vs a panel of tyrosine and serine-threonine kinases.

• 定義

  ChEBI: A member of the class of indolones that is 1,3-dihydro-2H-indol-2-one which is substituted by a (2,6-dichlorobenzyl)sulfonyl group at position 5 and by a (1H-pyrrol-2-yl)methylidene group at position 2, the pyrrole rin of which is substituted by methyl groups at positions 3 and 5, and by a [2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]carbonyl group at position 4 (the Z,R isomer).

• 生物活性

  Potent, selective and ATP-competitive inhibitor of MET kinase (IC 50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKB α , p38 α , MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.

PHA-665752 生産企業

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PHA-665752 スペクトルデータ(¹HNMR)

477575-56-7, PHA-665752 キーワード