I-BET567
目录号: PL13505 纯度: ≥99%
CAS No. :1887237-54-8
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中文名称
I-BET567
英文名称
I-BET567
英文别名
6-Quinolinecarboxamide, 1-acetyl-4-[(5-chloro-2-pyrimidinyl)amino]-1,2,3,4-tetrahydro-2-methyl-, (2S,4R)-;I-BET567
Cas No.
1887237-54-8
分子式
C17H18ClN5O2
分子量
359.81
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
I-BET567 是一种有效、具有口服活性 pan-BET 候选抑制剂,对 BRD4 BD1 和 BD2 的 pIC50s 分别为 6.9 和 7.2。I-BET567 已在肿瘤和炎症小鼠模型中已被证明有效。
生物活性
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC 50 s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.
性状
Solid
IC50 & Target[1][2]
BRD4 (BD1) 6.9 (pIC50) BRD2 7.2 (pIC
体外研究(In Vitro)
I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC50 6.2 (0.63 μM). has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
I-BET567 (compound 27) (3, 10, and 30 mg/kg; p.o.; once daily for 20 days) leads to a significant reduction in tumor growth compared with vehicle controls at both 10 and 30 mg/kg.
Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle dog.
species dose iv/po (mg/kg)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Humphreys PG, et al. Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate [published online ahead of print, 2022 Jan 7].
溶解度数据
In Vitro: DMSO : 100 mg/mL (277.92 mM; Need ultrasonic)配制储备液
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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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