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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-mTOR-eALM1137
eALM1137

Chemical Structure : eALM1137

CAS No.: 3134761-40-0

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eALM1137 (eALM-1137)

货号: PC-26526Not For Human Use, Lab Use Only.

eALM1137 is a highly potent, selective mTOR inhibitor with IC50 of 4.8 nM, weakly inhibits DNA-PK with IC50 of 77 nM (17-fold selectivity).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    eALM1137 is a highly potent, selective mTOR inhibitor with IC50 of 4.8 nM, weakly inhibits DNA-PK with IC50 of 77 nM (17-fold selectivity).
    eALM1137 shows antiproliferative activity against GBM cell lines: U87-MG and T98G with IC50 of 5.1 nM and 11 nM.
    eALM1137 does not inhibit PI3Kα, PKN3, CK1δ.
    eALM1137 demonstrates dose-dependent dual inhibition of mTORC1 and mTORC2 activities, as shown by the reduction of S6 and Akt phosphorylation, respectively, at 30 nM and higher concentrations, in T98G and U87-MG cells.
    eALM1137 treatment induces significant reduction in cell proliferation with an EC50 of 85 nM in triple mutant NPE cell line, which has a double deletion of NF1 and PTEN, and overexpression of EGFR in neural stem cells.
    eALM1137 inhibits mTORC1 signaling, as evidenced by reduced phosphorylation of the S6 ribosomal protein (Ser235/236 and Ser240/244) and 4E-BP1 (Thr37/46).

    物理化学性质&存储条件

    分子量 450.50
    分子式 C22H26N8O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    Isopropyl 4-((4-amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)piperidine-1-carboxylate

    参考文献

    1. Lorente-Macías Á, et al. J Med Chem. 2026 Apr 12. doi: 10.1021/acs.jmedchem.6c00541.

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