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AZD 3147

AZD 3147 是一种 mTORC 抑制剂，对 mTORC1 和 mTORC2 的 IC50 分别为 40.7 和 5.75 nM。 AZD 3147 对 PI3Kα、PI3Kβ、PI3Kδ 和 PI3Kγ 的 IC50 值分别为 912、5495、9333 和 6310 nM。

CAS号

1101810-02-9

分子式

C24H31N5O4S2

主要靶点

mTOR

仅限科研使用

Cat No : CM10486

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Synonyms

AZD 3147|AZD3147|AZD-3147|mTORC1|mTORC2

验证数据展示

  • CAS No.: 1101810-02-9

    AZD 3147
    CAS#: 1101810-02-9

产品信息

AZD 3147 is an inhibitor of mTORC with IC50s of 40.7 and 5.75 nM for mTORC1 and mTORC2. AZD 3147 shows IC50s of 912, 5495, 9333, and 6310 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively.

CAS号 1101810-02-9
分子式 C24H31N5O4S2
主要靶点 mTOR
主要通路 PI3K/Akt/mTOR 信号通路
分子量 517.66
纯度 99.99%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 AZD 3147|AZD3147|AZD-3147|mTORC1|mTORC2

体内活性

AZD3147在小鼠体内表现出的药代动力学参数包括清除率（CL）为78 mL/min/kg，稳态分布体积（Vss）为2.3 L/kg，半衰期（t1/2）为0.9小时，以及生物利用度（F）为61%[1]。

体外活性

在NIH3T3细胞中，AZD3147（1.5-50 nM）减轻了FGF介导的纤毛伸展[2]。AZD3147抑制神经母细胞瘤细胞系Kelly（IC50 = 0.88 nM）和IMR-32（IC50 = 662.4 nM）的细胞活力[3]。

溶解度

Ethanol:1 mg/mL (1.93 mM);DMSO:46.8 mg/mL (90.41 mM);Hydrochloride acid:100 mg/mL (193.18 mM)

参考文献

1.Pike, K.G., Morris, J., Ruston, L., et al. Discovery of AZD3147: A potent, selective dual inhibitor of mTORC1 and mTORC2. J. Med. Chem. 58(5), 2326-2349 (2015). AZD 3147
2.Michaela Kunova Bosakova, et al. Regulation of ciliary function by fibroblast growth factor signaling identifies FGFR3-related disorders achondroplasia and thanatophoric dysplasia as ciliopathies. Hum Mol Genet. 2018 Mar 15;27(6):1093-1105.
3.Rebecca Waetzig, et al. Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. Int J Med Sci. 2021 Jan 1;18(1):137-149.

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