Voruciclib|1000023-04-0|-陌孚医药/Medlife

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Voruciclib

目录号: PL02655 纯度: ≥99%

CAS No. :1000023-04-0

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中文名称	Voruciclib
英文名称	Voruciclib
英文别名	VORUCICLIB;2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one;2-[2-Chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4H-1-benzopyran-4-one;UNII-W66XP666AM;2-(2-chloro-4-(trifluoromethyl)phenyl)-5,7-dihydroxy-8-((2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4H-chromen-4-one;A14392;2-[2-Chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2S,3S)-2-(hydroxymethyl)-1-methylpyrrolidin;Voruciclib
Cas No.	1000023-04-0
分子式	C₂₂H₁₉ClF₃NO₅
分子量	469.84
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Voruciclib 是一种具有口服活性和选择性 CDK 抑制剂，K_i 为 0.626 nM-9.1 nM。Voruciclib 可以有效阻断 MCL-1 的转录调节子 CDK9。Voruciclib 抑制多种弥漫性大 B 细胞淋巴瘤 (DLBCL) 模型中 MCL-1 的表达。

生物活性

Voruciclib is an orally active and selective CDK inhibitor with K i values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).

性状

Solid

IC50 & Target[1][2]

CDK9/cyc T2 0.626 nM (Ki) CDK9/CycT1 1.68 nM (Ki)p

体外研究(In Vitro)

Voruciclib (0.5-5 μM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes.
Ki values for each target such as CDK9/cyc T2, CDK9/cyc T1, CDK6/cyc D1, CDK4/cyc D1, CDK1/cyc B, and CDK1/cyc A for Voruciclib hydrochloride are 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, 9.1 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

体内研究(In Vivo)

Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL. 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]. Dey J, et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition. Sci Rep. 2017 Dec 21;7(1):18007.

溶解度数据	In Vitro: DMSO : 50 mg/mL (106.42 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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