1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン

1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン 化学構造式
172889-27-9
CAS番号.
172889-27-9
化学名:
1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン
别名:
1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン;PP2
英語名:
PP2
英語别名:
PP2;CS-717;AG 1879;AGL 1879;PP2(AG 1879);PP2(AGL 1879);AG 1879,AGL 1879;PP2;AGL 1879;PP 2;PP-2;PP 2 (enzyme inhibitor);Src kinase inhibitor PP2
CBNumber:
CB1406580
化学式:
C15H16ClN5
分子量:
301.77
MOL File:
172889-27-9.mol

1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン 物理性質

沸点 :
493.5±40.0 °C(Predicted)
比重(密度) :
1.35±0.1 g/cm3(Predicted)
貯蔵温度 :
2-8°C
溶解性:
DMSO (最大 25mg/ml) またはエタノール (加熱すると最大 3mg/ml) に可溶。
酸解離定数(Pka):
3.96±0.30(Predicted)
外見 :
オフホワイトの無地
色:
オフホワイト
安定性::
購入日から2年間安定です。この DMSO またはエタノール溶液は、-20°C で 1 か月間保存できます。
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  T
Rフレーズ  25
Sフレーズ  45
RIDADR  UN 2811 6.1 / PGIII
絵表示(GHS) GHS hazard pictograms
注意喚起語 危険
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H301 飲み込むと有毒 急性毒性、経口 3 危険 GHS hazard pictograms P264, P270, P301+P310, P321, P330,P405, P501
注意書き
P301+P310 飲み込んだ場合:直ちに医師に連絡すること。

1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン 価格 もっと(6)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01BVI1767-5
PP2
172889-27-9 5mg ¥100100 2020-09-21 購入
富士フイルム和光純薬株式会社(wako) W01BVI1767-1
PP2
172889-27-9 1mg ¥26000 2020-09-21 購入
富士フイルム和光純薬株式会社(wako) W01TOC1407 PP2
PP 2
172889-27-9 10mg ¥101000 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01MAS096440 1-(tert-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-d]ピリミジン-4-アミン
1-(tert-Butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
172889-27-9 250mg ¥1043300 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01MAS096440 1-(tert-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-d]ピリミジン-4-アミン
1-(tert-Butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
172889-27-9 1g ¥2318400 2024-03-01 購入

1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン 化学特性,用途語,生産方法

外観

結晶~粉末

溶解性

メタノール、DMSOに溶ける。

用途

チロシンキナーゼの研究。

説明

The Src family of non-receptor tyrosine kinases regulate cell adhesion, growth, and differentiation through activation of multiple intracellular signaling pathways. Normally inactive, Src kinases are transiently activated during mitosis and constitutively activated by abnormal mutations. PP2 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. It inhibits p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM), and Src (IC50 = 100 nM). PP2 does not significantly affect the activity of EGFR kinase (IC50 = 480 nM), JAK2 (IC50 > 50 μM), or ZAP-70 (IC50 > 100 μM). PP2 inhibits the activation of focal adhesion kinase as well as its phosphorylation at Tyr577. PP2 also inhibits anti-CD3-stimulated tyrosine phosphorylation of human T-cells with an IC50 value of 600 nM.

使用

PP2 has been used:
  • to analyze the effects of Src/focal adhesion kinase (FAK) signaling on IQ domain GTPase-activating protein 1 (IQGAP1)-mediated anoikis resistance
  • for Src inhibition to study its effect on epidermal growth factor receptor (EGFR) and nuclear factor erythroid 2-related factor 2 (Nrf2) phosphorylation in non-small cell lung cancer (NSCLC) cells
  • for pharmacological inhibition of SRC in MDA-MB-231 breast cancer cells

生物活性

Selective inhibitor of Src-family tyrosine kinases. Inhibits p56 lck and p59 fynT (IC 50 values are 4 and 5 nM respectively). Displays > 10000-fold selectivity over ZAP-70 and JAK2. Moderately inhibits CSK (IC 50 = 0.73 μ M).

酵素阻害剤

This cell-permeable and photosensitive ATP site-directed pyrazolepyrimidine (FW = 301.78 g/mol), also known as 4-amino-5-(4- chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine and tyrphostin AG 1879, potently inhibits Lck and Fyn protein kinases, with IC50 values of 4 nM and 5 nM. PP2 is ~100x less potent toward EGFR and is inactive for ZAP-70, JAK2 and PKA. PP2 prevented serum-independent growth of RET/PTC1-transformed NIH3T3 fibroblasts and of TPC1 and FB2, two human papillary thyroid carcinoma cell lines that carry spontaneous RET/PTC1 rearrangements. PP2 activates the E-cadherin-mediated cell adhesion system, suppressing metastasis in cancer cells. In cervical cancer cells (HeLa and SiHa), 10 μM PP2 down-regulates pSrc-Y416, pEGFR-Y845, and pEGFR-Y1173 expression levels, while downregulatING pSrc-Y416 and pEGFR-Y845, but not pEGFR-Y1173. PP2 is also a potential neuroprotective agent in cerebral ischemia-reperfusion. Target(s): casein kinase 1d, IC50 = 1.3 μM; Csk protein-tyrosine kinase; focal adhesion kinase; lymphocyte kinase, IC50 = 0.06 μM; p56lck, IC50 = 4 nM; p59fynT, IC50 = 5 nM; receptor proteintyrosine kinase; src protein-tyrosine kinase, IC50 = 0.7 μM (5,11,12- 23); stress-activated protein kinase 2a/p38, IC50 = 1.4 μM; and Yes kinase.

1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン 上流と下流の製品情報

原材料

準備製品


1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン 生産企業

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1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン  スペクトルデータ(1HNMR)


172889-27-9(1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン)キーワード:


  • 172889-27-9
  • [1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-yl]amine
  • 1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine
  • PP2(AG 1879)
  • AGL 1879
  • PP 2 (enzyme inhibitor)
  • Src kinase inhibitor PP2
  • 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-
  • AG 1879,AGL 1879
  • 3-(4-Chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine AGL 1879
  • 4-Amino-3-(4-chlorophenyl)-1-(t-butyl)-1H-pyrazolo[3,4-d]pyrimidine
  • PP2;AGL 1879;PP 2;PP-2
  • 1-(TERT-BUTYL)-3-(4-CHLOROPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE
  • 1-(TERT-BUTYL)-3-(4-CHLOROPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE
  • 3-(4-CHLOROPHENYL) 1-(1,1-DIMETHYLETHYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE
  • 4-AMINO-5-(4-CHLOROPHENYL)-7-(T-BUTYL)PYRAZOLO[3,4-D]PYRIMIDINE
  • 4-AMINO-5-(4-CHLOROPHENYL)-7-(TERT-BUTYL)PYRAZOLO[3,4-D]PYRIMIDINE
  • AG 1879
  • 3-(4-Chlorophenyl)-1-(1,1-dimethylethyl)-(1H)-pyrazolo[3.4-d]pyrimidine-4-amine
  • PP2
  • PP 2;AG1879;AG 1879;AGL 1879
  • PP2(AGL 1879)
  • CS-717
  • 7-tert-butyl-5-(4-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
  • Src family kinase inhibitor PP2
  • 1-(TERT-ブチル)-3-(4-クロロフェニル)-1H-ピラゾロ[3,4-D]ピリミジン-4-アミン
  • PP2
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