製品コードS1093 別名:GSK 4529



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。

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JPY 82502.00 あり


  • (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。
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
25 nM 27 nM

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]

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>


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]




+ 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.


+ 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)



+ 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

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。


分子量 851.96


CAS No. 1089283-49-7
別名 GSK 4529





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


  • マス




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


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

  • C1



  • 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):




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


マス 濃度 ボリューム 分子量



Handling Instructions


  • * 必須


IGF-1R Inhibitors with Unique Features


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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID