GSK1904529A

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GSK1904529A  纯度: 99.22%

GSK1904529A 是一种有效的，选择性的，具有口服活性和 ATP 竞争性的胰岛素样生长因子 1 受体 (IGF-1R) 和胰岛素受体 (IR) 抑制剂，IC50 值分别为 27 和 25 nM。GSK1904529A 在其他 45 种丝氨酸/苏氨酸和酪氨酸激酶中显示出较弱的活性 (IC50>1 μM)。GSK1904529A 具有抗肿瘤活性。

GSK1904529A

GSK1904529A Chemical Structure

CAS No. : 1089283-49-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1270 In-stock
10 mg ￥1350 In-stock
50 mg ￥3450 In-stock
100 mg ￥6250 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity[1][2].

IC50 & Target

IC50: 27 nM (IGF-1R), 25 nM (IR)[1]
体外研究
(In Vitro)

GSK1904529A displays high affinities for IGF-1R and IR, with Kis of 1.6 and 1.3 nM, respectively[1].
GSK1904529A (72 h) inhibits tumor cells proliferation with IC50s ranges from 35 nM to >30 μM, and Ewing’s sarcoma and multiple myeloma cell lines are greatest sensitive[1].
GSK1904529A (0.03-3 μM; 24 and 48 h) arrests cells at the G1 phase of the cell cycle[1].
GSK1904529A (2 h) inhibits phosphorylation of IGF-IR and IR with IC50s of 22 and 19 nM in NIH-3T3/LISN and NIH-3T3-hIR cells, respectively[1].
GSK1904529A (0.01-3 μM; 4 h) blocks the major downstream signal transduction pathways mediated by IGF-IR and IR in NIH-3T3/LISN and NIH-3T3-hIR cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: COLO 205, MCF-7, and NCI-H929 cells
Concentration: 0, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time: 24 and 48 hours
Result: Increased the accumulation in G1 and decreased accumulation in S and G2-M phases of the cell cycle.

Western Blot Analysis[1]

Cell Line: NIH-3T3/LISN and NIH-3T3-hIR cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time: 4 hours
Result: Inhibited the ligand-induced phosphorylation of IGF-IR and IR at concentrations >0.01 μM.
Decreased the phosphorylation of AKT, IRS-1, and ERK.

体内研究
(In Vivo)

GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice[1].
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice[1].
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nu/nu CD-1 mice are bring NIH-3T3/LISN tumor[1]
Dosage: 30 mg/kg
Administration: P.o. once or twice daily for 21 d
Result: Resulted in 56% (once daily) and 98% (twice daily) inhibition of tumor growth.
No significant decrease in body weight on the once-daily schedule.
Observed 11-13% of body weight loss, and recovered to near baseline 6 days after the cessation of treatment in twice-daily group.

分子量

851.96

Formula

C44H47F2N9O5S
CAS 号

1089283-49-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (58.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1738 mL 5.8688 mL 11.7376 mL
5 mM 0.2348 mL 1.1738 mL 2.3475 mL
10 mM 0.1174 mL 0.5869 mL 1.1738 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (3.23 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (3.23 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Sabbatini P, et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin Cancer Res, 2009, 15(9), 3058-3067.

    [2]. Zhou Q, et, al. GSK1904529A, an insulin-like growth factor-1 receptor inhibitor, inhibits glioma tumor growth, induces apoptosis and inhibits migration. Mol Med Rep. 2015 Sep;12(3):3381-3385.

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