GSK1904529A

製品コードS1093 別名:GSK 4529

GSK1904529A化学構造

分子量(MW):851.96

GSK1904529Aは一種の選択性的なIGF-1RとIRの阻害剤で、無細胞実験でこのIC50値が27 nMと25 nMです。GSK1904529Aは、IGF-1R/InsRに作用する選択性はAkt1/2、Aurora A/B、B-Raf、CDK2、EGFR等に作用する選択性より100倍以上が高くなります。

サイズ 価格(税別) 在庫  
JPY 81340.00 あり
JPY 32702.00 あり
JPY 82502.00 あり

カスタマーフィードバック(4)

  • (E) The level of migration ability of HEC-1B cells treated with insulin, GSK1904529A, and the silencing of DHCR24 was determined using a transwell assay. (F) The invasion ability of HEC-1B cells treated with insulin, GSK1904529A, and silencing of DHCR24 was probed. The data are presented as the mean ± SD of three independent experiments. (*p < 0.05; **p < 0.01; ***p < 0.001).

    Sci Rep, 2017, 7:41404. GSK1904529A purchased from Selleck.

    Inhibition of IGF-1 induced IGF-1R phosphorylation by GSK1904529A. A549 cells were serum-starved O/N and pre-incubated for 4 h with 5 μM GSK1904529A, followed by stimulation with 50ng/ml IGF-1. + IGF-1: positive control; -S: negative control.

    Dr. Ursula Broder from Institut. GSK1904529A purchased from Selleck.

  • Immortalized wild-type mouse embryonic fibroblasts were serum starved for 4 hours, then stimulate with 100ng/ml IGF-1 for 5 min. Inhibitor was added for the last 1 hour of serum starvation.

     

     

    Xuejun Jiang from Memorial Sloan-Kettering Cancer Center. GSK1904529A purchased from Selleck.

    Dose response curve of compound on melanoma cell lines.  Compound was dissolved in DMSO, added in a 5-fold dilution series, starting with 10 μM, and incubated for 72 hours.  Fluorescence was measured after 8 hours incubation in resazurin.  Data was normalized to DMSO (maximal viability) and Doxorubicin (minimum viability).

    One customer. GSK1904529A purchased from Selleck.

製品安全説明書

IGF-1R阻害剤の選択性比較

生物活性

製品説明 GSK1904529Aは一種の選択性的なIGF-1RとIRの阻害剤で、無細胞実験でこのIC50値が27 nMと25 nMです。GSK1904529Aは、IGF-1R/InsRに作用する選択性はAkt1/2、Aurora A/B、B-Raf、CDK2、EGFR等に作用する選択性より100倍以上が高くなります。
ターゲット
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
25 nM 27 nM
体外試験

GSK1904529A is a reversible, ATP-competitive inhibitor and has enzyme-inhibitor binding values against IGF-1R and IR with Ki of 1.6 nM and 1.3 nM, respectively. GSK1904529A potently inhibits the ligand-induced phosphorylation of IGF-1R and IR at concentrations above 0.01 μM, followed by blocking downstream signaling (AKT, IRS-1, and ERK). GSK1904529A potently inhibits NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES RD-ES cells with IC50 of 60 nM, 35 nM, 43 nM, 61 nM and 62 nM, respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines including NCI-H929, MOLP-8, LP-1 and KMS-12-BM etc. GSK1904529A induces cell cycle arrest at the G1 phase in cell lines COLO 205, MCF-7, and NCI-H929, which are sensitive to GK1904529A. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NIH3T3 cells MVLGeY5kfGmxbjDhd5NigQ>? NIfhcVdKdmirYnn0bY9vKG:oIHj1cYFvKGmwc4XsbY4hemWlZYD0c5Ih[XW2b4Doc5NxcG:{eXzheIlwdiCrbjD0doFve2[nY4Tl[EBud3W|ZTDOTWg{XDNiY3XscJMtKEmFNUC9NVkhdk1? NF3SVW8yQTFyMUG0Ny=>
human TC71 cells NIDETY1Rem:uaX\ldoF1cW:wIHHzd4F6 NXTO[GM3PzJiaB?= M4jvR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVFO3NUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscJRqfGW{IHHzd4F6NCCLQ{WwQVM2KG6P MVSxPVExOTF2Mx?=
human SK-ES cells NVHkcpl1WHKxbHnm[ZJifGmxbjDhd5NigQ>? NIPTTmI4OiCq MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVXTJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzseIl1\XJiYYPzZZktKEmFNUC9OlEhdk1? MoLkNVkyODFzNEO=
human NCI-H929 cells M4\2VXBzd2yrZnXyZZRqd25iYYPzZZk> NIe1fFM4OiCq M{nSTmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg6OjliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGy2aYTldkBie3OjeTygTWM2OD16MTDuUS=> NVTmVlNxOTlzMEGxOFM>
human LP-1 cells NHT2boFRem:uaX\ldoF1cW:wIHHzd4F6 NHjkXIw4OiCq MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEySLUGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHz0bZRmeiCjc4PhfUwhUUN3ME2xNFQhdk1? NV;qOmRPOTlzMEGxOFM>
human COLO205 cells NWHRUphKWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{TJSlczKGh? Ml6yRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPNlA2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtfGm2ZYKgZZN{[XluIFnDOVA:OTJ2IH7N NVvifoxFOTlzMEGxOFM>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 GSK1904529A indicates 98% tumor growth inhibition in NIH-3T3/LISN tumor-bearing mice at a dose of 30 mg/kg (orally, twice-daily) and 75% in COLO 205 xenografts mice (once daily). Among HT29 and BxPC3 xenografts, GSK1904529A produces moderate tumor growth inhibition with no side effects at a dose of 30 mg/kg. Meanwhile, GSK1904529A shows minimal effects on blood glucose levels. GSK1904529A (~3.5 μM in blood) completely inhibits IGF-1R phosphorylation. GSK1904529A has been implicated in treatment of various IGF-1R-dependent tumors including prostate, colon, breast, pancreatic, ovarian, and sarcomas. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

Kinase assays:

GSK1904529A is dissolved in DMSO as stock solution at 10 mM. Baculovirus-expressed glutathione S-transferase-tagged proteins encoding the intracellular domain of IGF-1R (amino acids 957-1367) and IR (amino acids 979-1382) are used for determination of IC50. Kinases are activated by preincubating the enzyme (2.7 μM final concentration) in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1mg/mL bovine serum albumin, and 2 mM ATP. GSK1904529A is diluted in DMSO and dispensed into the assay plates (100 nL/well). Kinase reactions contained (in 10 μL) 50 mM HEPES (pH 7.5), 3 mM DTT, 0.1mg/mL bovine serum albumin, 1mM CHAPS, 10 mM MgCl2, 10 μM ATP, 500 nM substrate peptide (biotin-aminohexylAEEEEYMMMMAKKKK-NH2; QPC), and 0.5 nM activated enzyme. Reactions are stopped after 1 hour at room temperature with 33 μM EDTA. Peptide phosphorylation is measured by time-resolved fluorescence resonance energy transfer with 7 nM streptavidin Surelight allophycocyanin and 1nM europium-conjugated phosphotyrosine antibodies. Plates are read in a multilabel reader.
細胞試験:

[1]

+ 展開
  • 細胞株: Tumor cell lines including multiple myeloma, ewing's sarcoma, askin's tumor, colon, breast, anaplastic large cell lymphoma, lung, cervix, head and neck, prostate and ovary.
  • 濃度: ~ 100 μM, stocked in DMSO at 10 mM.
  • 反応時間: 72 hours
  • 実験の流れ:

    Cells are seeded in 96-well plates and incubated overnight at 37 °C, and treated with various concentrations of GSK1904529A for 72 hours. For the NIH-3T3/LISN, cells are seeded on collagen-coated 96-well tissue culture plates and allowed to adhere for 24 hours. The tissue culture medium is replaced with serum-free medium and the cells are treated with DMSO or GSK1904529A for 2 hours. IGF-I (30 ng/mL) is added and the cells are incubated at 37 °C for 72 hours. Cell proliferation is quantified using the CellTiter-Glo Luminescent Cell Viability Assay. IC50 values are determined.(参考用のみ)

動物試験:

[1]

+ 展開
  • 動物モデル: NIH-3T3/LISN, COLO 205, HT29, and BxPC3 cells are implanted s.c. into the right flank of 8- to 10-wk-old female nu/nu CD-1athymic mice.
  • 製剤: Formulated in 20% sulfobutylether-h-cyclodextrin (pH 3.5; ISP)
  • 投薬量: ~30 mg/kg
  • 投与方法: Orally administered
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 124 mg/mL (145.54 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 851.96
化学式

C44H47F2N9O5S

CAS No. 1089283-49-7
保管
別名 GSK 4529

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

IGF-1R信号経路図

IGF-1R Inhibitors with Unique Features

相関IGF-1R製品

Tags: GSK1904529Aを買う | GSK1904529A ic50 | GSK1904529A供給者 | GSK1904529Aを購入する | GSK1904529A費用 | GSK1904529A生産者 | オーダーGSK1904529A | GSK1904529A化学構造 | GSK1904529A分子量 | GSK1904529A代理店
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID