CB-103|218457-67-1|(CB-103)-陌孚医药/Medlife

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CB-103 (Synonyms: CB-103)

目录号: PL07870 纯度: ≥99%

CAS No. :218457-67-1

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中文名称	CB-103
中文别名	5-氨基-2-(4-叔丁苯氧基)吡啶;6-[4-(叔丁基)苯氧基]吡啶-3-胺
英文名称	CB-103
英文别名	6-(4-(tert-Butyl)phenoxy)pyridin-3-amine;3-Pyridinamine,6-[4-(1,1-dimethylethyl)phenoxy]-;5-Amino-2-(4-tert-butylphenoxy)pyridine;6-(4-tert-butylphenoxy)pyridin-3-amine;CB-103;6-[4-(tert-butyl)phenoxy]pyridin-3-amine;Q5BB91JL0V;MLS000833648;CB103;6-(4-tert-butylphenoxy)-3-pyridinamine;SMR000457169;Maybridge1_001148;Oprea1_231562;BDBM87327;cid_2735289;GTPL10517;HMS544M04;REGID_for_CID_2735289;HMS2787I06;NSC823659;s9719
Cas No.	218457-67-1
分子式	C₁₅H₁₈N₂O
分子量	242.32
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

CB-103 是一种首创的，有口服活性的蛋白相互作用 (PPI) 抑制剂，靶向 NOTCH 转录复合体，具有抗肿瘤活性。

生物活性

CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.

性状

Solid

IC50 & Target[1][2]

notch signaling pathway

体外研究(In Vitro)

CB-103 acts as a pan-NOTCH inhibitor by targeting NOTCH transcriptional activation complex.
CB-103 can block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines.
CB-103 exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

体内研究(In Vivo)

CB-103 inhibits NOTCH dependent cellular processes in mice.
CB-103 blocks in vivo growth of PDX models of T-ALL.
CB-103 (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer.
CB-103 exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors.
has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Freddy Radtke, et al. Inhibitors of notch signalling pathway and use thereof in treatment of cancers. US9296682B2.
[2]. R.Lehal, et al. Development of a novel first-in-class oral inhibitor of the NOTCH pathway.
[3]. Rajwinder Lehal, et al. Non clinical pharmacology, pharmacokinetics and safety profiling of CB-103: A novel first-in-class small molecule inhibitor of the NOTCH pathway.

溶解度数据	In Vitro: DMSO : 100 mg/mL (412.68 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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