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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Notch-CB-103
CB-103

Chemical Structure : CB-103

CAS No.: 218457-67-1

CB-103 (CB103)

货号: PC-38257Not For Human Use, Lab Use Only.

CB-103 (CB103) is an orally active small-molecule inhibitor of the Notch transcription activation complex, inhibits both ligand-dependent and ligand-independent Notch activation in cell-based assays (IC50=0.9-3.9 uM).

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100 mg ¥880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CB-103 (CB103) is an orally active small-molecule inhibitor of the Notch transcription activation complex, inhibits both ligand-dependent and ligand-independent Notch activation in cell-based assays (IC50=0.9-3.9 uM).
CB-103 does not inhibit Wnt or Hedgehog signaling using reporter assays.
CB-103 inhibits Notch signaling in primary human T cell acute lymphoblastic leukemia and other Notch-dependent human tumor cell lines, and concomitantly induces cell cycle arrest and apoptosis, thereby impairing proliferation, including in GSI-resistant human tumor cell lines with chromosomal translocations and rearrangements in Notch genes.
CB-103 produces Notch loss-of-function phenotypes in flies and mice. CB-103 inhibits the growth of human breast cancer and leukemia xenografts, notably without causing the dose-limiting intestinal toxicity associated with other Notch inhibitors.

物理化学性质&存储条件

分子量 242.322
分子式 C15H18N2O
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

100 mM in DMSO (24 mg/mL)

Chemical Name/SMILES

6-(4-(tert-butyl)phenoxy)pyridine-3-amine

参考文献

1. Lehal R, et al. Proc Natl Acad Sci U S A. 2020 Jul 14;117(28):16292-16301.

2. Lue JK, et al. Ann Lymphoma. 2020 Sep 30;4:7.

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