2. Epigenetics
  3. Epigenetic Reader Domain
  4. KWZL-7f15

KWZL-7f15 (compound 7f15) 是一种双重 CDK6/BET 抑制剂，对人源 CDK6 的 IC50 为 31.81 nM。KWZL-7f15 可抑制 CDK6-RB 轴与 BRD4-Myc 轴。KWZL-7f15 对三阴性乳腺癌细胞具有抗增殖活性。KWZL-7f15 在异种移植小鼠模型中展现出抗肿瘤活性，且无显著不良反应。KWZL-7f15 可用于三阴性乳腺癌的相关研究。

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KWZL-7f15

KWZL-7f15 Chemical Structure

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KWZL-7f15 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KWZL-7f15 (compound 7f15) is a dual CDK6/BET inhibitor with an IC50 of 31.81 nM against human CDK6. KWZL-7f15 inhibits the CDK6-RB axis and the BRD4-Myc axis. KWZL-7f15 exhibits antiproliferative activity against triple-negative breast cancer cells. KWZL-7f15 shows antitumor activity in xenograft mouse models without significant adverse effects. KWZL-7f15 can be used in studies related to triple-negative breast cancer[1].

体外研究
(In Vitro)

KWZL-7f15 (compound 7f15) 对三阴性乳腺癌 (TNBC) 细胞株 MDA-MB-231 (IC50 = 0.35 μM)、BT-549 (IC50 = 2.77 μM) 表现出强细胞毒性，且对正常乳腺上皮细胞 MCF-10A 的 IC50 > 30 μM，具有高选择性[1]。
KWZL-7f15 (500 nM for CDK4/CycD1 and CDK6/CycD3) 是一种泛 BET 及选择性 CDK4/CDK6 抑制剂，其 IC50 值分别为 31.81 nM (CDK6)、56.41 nM (BRD4)、37.30 nM (BRD2 BD1+BD2)、34.02 nM (BRD3 BD1+BD2)、31.79 nM (BRD4 BD2)；在 500 nM 条件下对 CDK4/CycD1 的抑制率为 57.73%，对 CDK6/CycD3 的抑制率为 80.53%[1]。
KWZL-7f15 经细胞热位移实验证实可在 MDA-MB-231 细胞中直接结合 CDK6 和 BRD4，提高二者的热稳定性[1]。
KWZL-7f15 可调控 MDA-MB-231 细胞中的蛋白表达，导致 BRD4、c-Myc、p-Rb 及 Bcl2 呈剂量和时间依赖性下调，同时使 Bax 及活化型半胱天冬酶 3 (cleaved-caspase 3) 上调[1]。
KWZL-7f15 (0.25-1 μM; 48 h) 以剂量依赖的方式诱导 MDA-MB-231 细胞发生 G0/G1 期阻滞[1]。
KWZL-7f15 可在 MDA-MB-231 细胞中诱导氧化应激与 DNA 损伤，具体表现为升高细胞内 ROS 水平、上调 γ-H2AX、抑制 RAD51 并诱导 DNA 链断裂[1]。
KWZL-7f15 (0.25 μM) 可在划痕愈合实验中抑制 MDA-MB-231 细胞的迁移[1]。
KWZL-7f15 (0.25 μM) 可抑制 MDA-MB-231 细胞的集落形成[1]。
KWZL-7f15 通过将嘧啶-NH-吡啶基序插入铰链区并与 ASP104 形成额外氢键，与 CDK6 (PDB: 5L2S) 结合；同时通过二氢喹喔啉酮母核占据疏水口袋，与 TYR97、ASN140 形成氢键，并与 PRO86、GLN85 形成水桥相互作用以增强结合亲和力，从而与 BRD4 (PDB: 6JI5) 结合[1]。

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

KWZL-7f15 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.25-1 μM
Incubation Time: 48 h
Result: Induced G0/G1 phase arrest in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 1 μM
Incubation Time: 48 h
Result: Promoted caspase-dependent apoptosis.
Reversed cytotoxicity when co-treated with pan-caspase inhibitor Z-VAD-FMK.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax AUC0-t T1/2 Vd CL MRT0-∞
Rat[1] 5 mg/kg i.p. 160.60 ng/mL 6.00 h 2114.18 13.06 h 420.19 L/kg 22.84 L/h/kg 20.73 h
体内研究
(In Vivo)

KWZL-7f15 (compound 7f15) (腹腔注射；每日 1 次；连续 14 天，剂量 20-40 mg/kg) 在 BALB/c 裸鼠 MDA-MB-231 异种移植模型中表现出剂量依赖性的体内抗肿瘤活性，在 40 mg/kg (腹腔注射，每日 1 次，连续 14 天) 剂量下的肿瘤生长抑制率达 84.69%，且无明显全身毒性[1]。

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

Animal Model: BALB/c nude (female, 4−5 weeks old, 18−20 g, subcutaneous xenograft model via MDA-MB-231 tumor cell implantation)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; daily; 14 days
Result: Produced a tumor growth inhibition (TGI) rate of 61.64% at 20 mg/kg.
Produced a TGI rate of 84.69% at 40 mg/kg, which was higher than the TGI rate of the Abemaciclib + BQ0 combination control.
Caused no significant body weight loss.
Showed no treatment-related lesions in heart, liver, spleen, lung, and kidney via histopathological analysis.
Reduced positive expression of c-Myc and p-Rb significantly in tumor tissues compared to the control group via immunohistochemical analysis.
分子量

490.58

Formula

C26H31FN8O
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

KWZL-7f15 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

KWZL-7f15Epigenetic Reader DomainBRD4triple-negative breast cancerRB axisBT-549CDK6Myc axisCDK4MDA-MB-231BETMCF-10AInhibitorinhibitorinhibit

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