2. Cell Cycle/DNA Damage Apoptosis
  3. DNA/RNA Synthesis CDK Apoptosis
  4. Enitociclib

Enitociclib  (Synonyms: BAY-1251152; VIP152)

目录号: HY-103019E
产品使用指南 技术支持

Enitociclib (BAY-1251152; VIP152) 是一种选择性 CDK9 抑制剂和凋亡 (apoptosis) 诱导剂。Enitociclib 通过抑制 CDK9 活性，减少 RNA 聚合酶 Pol II 羧基末端结构域 (CTD) 丝氨酸2 (Ser2) 的磷酸化，从而下调 MYC、MCL1 等关键致癌基因的转录。Enitociclib 具有靶向 MYC+ 淋巴瘤和多发性骨髓瘤 (MM) 细胞的抗增殖活性，与 Bortezomib (HY-10227)、Lenalidomide (HY-A0003) 具有协同作用，可用于血液系统恶性肿瘤研究。

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Enitociclib Chemical Structure

Enitociclib Chemical Structure

CAS No. : 1610408-97-3

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规格 价格 是否有货 数量
1 mg ￥5840
1 - 2 周
5 mg 现货 1 - 2 周
10 mg 现货 1 - 2 周
50 mg   询价  
100 mg   询价  

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Customer Review

Enitociclib 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Enitociclib (BAY-1251152; VIP152) is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies[1][2].

IC50 & Target

CDK9

 

体外研究
(In Vitro)

Enitociclib (12.5-200 nM；96 h) 在多发性骨髓瘤 (MM) 细胞系 (NCI-H929、MM1.S、OPM-2、U266B1) 中呈浓度依赖性抑制细胞活力，IC50 为 36-78 nM[2]。
Enitociclib (0.5-1 μM；6-24 h) 在MM细胞系 (NCI-H929、OPM-2) 中诱导细胞凋亡，表现为凋亡标志物 caspase-3 和 PARP 的切割增加，同时下调抗凋亡蛋白 Mcl-1 和致癌蛋白 c-Myc 的表达[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Enitociclib 相关抗体:

Cell Viability Assay[2]

Cell Line: NCI-H929, MM1.S, OPM-2, U266B1
Concentration: 12.5-200 nM
Incubation Time: 96 h
Result: Reduced cell viability in a concentration-dependent manner, with IC50s ranging from 36 nM-78 nM across the tested cell lines.
体内研究
(In Vivo)

Enitociclib (15 mg/kg；静脉注射；每周 1 次；3 周) 在小鼠多发性骨髓瘤 (MM) 异种移植模型 (JJN-3、NCI-H929、OPM-2) 中显著抑制肿瘤生长，可减少肿瘤体积并延长小鼠生存时间[2]。
Enitociclib (15 mg/kg；静脉注射；每周 1 次) 与 Lenalidomide (HY-A0003) (50 mg/kg，口服，每日 1 次) 或 Bortezomib (HY-10227) (0.8 mg/kg，腹腔注射，每周 2 次) 联合使用，在 OPM-2 异种移植模型中协同抑制肿瘤生长，效果优于单因素处理组[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female SCID/Beige mice (6-8 weeks old) with JJN-3 xenografts; female NOD/SCID mice (6-8 weeks old) with NCI-H929 or OPM-2 xenografts[2]
Dosage: 15 mg/kg
Administration: Intravenous (IV) injection, once weekly, for 3 weeks
Result: Significantly reduced tumor volumes and prolonged survival compared to vehicle control.
In JJN-3 xenografts, single-dose treatment transiently inhibited transcription of MYC, MCL1, and PCNA, induced caspase-3 and PARP cleavage, and reduced c-Myc protein levels for up to 24 hours.
Clinical Trial
分子量

404.43

Formula

C19H18F2N4O2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Enitociclib 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Enitociclib1610408-97-3BAY-1251152 VIP152BAY1251152BAY 1251152VIP152VIP 152VIP-152DNA/RNA SynthesisCDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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