CB-103 is a γ-secretase inhibitor. 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 and inhibits the growth of human breast cancer and leukemia xenografts, notably without causing the dose-limiting intestinal toxicity associated with other Notch inhibitors.
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名称 | CB-103 |
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Iupac 化学名称 | 5-Amino-2-(4-tert-butylphenoxy)pyridine |
同义词 | CB-103; CB 103; CB103; |
英文同义词 | CB-103; CB 103; CB103; |
分子式 | C15H18N2O |
分子量 | 242.32 |
Smile | CC(C)(C)C1=CC=C(C=C1)OC2=NC=C(C=C2)N |
InChiKey | WHIWGRCYMQLLAO-UHFFFAOYSA-N |
InChi | InChI=1S/C15H18N2O/c1-15(2,3)11-4-7-13(8-5-11)18-14-9-6-12(16)10-17-14/h4-10H,16H2,1-3H3 |
Cas号 | 218457-67-1 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
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纯度 | 98% Min. |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
海关编码 |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Fabbro D, Bauer M, Murone M, Lehal R. Notch Inhibition in Cancer: Challenges and Opportunities. Chimia (Aarau). 2020 Oct 28;74(10):779-783. doi: 10.2533/chimia.2020.779. PMID: 33115560.
2: Lehal R, Zaric J, Vigolo M, Urech C, Frismantas V, Zangger N, Cao L, Berger A, Chicote I, Loubéry S, Choi SH, Koch U, Blacklow SC, Palmer HG, Bornhauser B, González-Gaitán M, Arsenijevic Y, Zoete V, Aster JC, Bourquin JP, Radtke F. Pharmacological disruption of the Notch transcription factor complex. Proc Natl Acad Sci U S A. 2020 Jul 14;117(28):16292-16301. doi: 10.1073/pnas.1922606117. Epub 2020 Jun 29. PMID: 32601208; PMCID: PMC7368267.