2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain c-Myc Apoptosis
  4. CFT-2718

CFT-2718 是一种选择性 CRBN 依赖型 BRD4 PROTAC 降解剂。CFT-2718 可介导 BRD4 快速、选择性降解，降低总 RPB1 及磷酸化 Ser2 RPB1 水平，并降低 MYC 蛋白水平。CFT-2718 能够抑制癌细胞增殖并诱导细胞凋亡 (apoptosis)。CFT-2718 可抑制肺癌和胰腺癌患者来源异种移植模型的生长。CFT-2718 可用于癌症相关研究，如小细胞肺癌和胰腺癌。

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CFT-2718

CFT-2718 Chemical Structure

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1 mg ￥3060
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CFT-2718 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer[1].

IC50 & Target[1]

BRD4

 

体外研究
(In Vitro)

CFT-2718 (0.01-1000 nM；3 h) 可在携带内源性标签 BRD4 的 293T 细胞中强效诱导 BRD4 降解，处理 3 小时后，在 10 nM 浓度下即可达到 90% 的降解率[1]。
CFT-2718 (0.01-1000 nM；72 h) 以浓度依赖的方式降低 MOLT4 CRBN+/+ 急性淋巴细胞白血病细胞的活力，在 10 nM 处理 72 h 后可杀伤约 75% 的细胞[1]。
CFT-2718 (0.1-10 nM；2 h) 可在 MOLT4 CRBN+/+ 细胞中诱导 CRBN 介导的快速、浓度依赖性 BRD4 降解[1]。
CFT-2718 (72 h) 以浓度依赖的方式降低小细胞肺癌 (SCLC) 和胰腺癌细胞系的活力，对 H69、H446、PNX-001 和 PNX-017 细胞的 IC50 值分别为 0.02、0.47、6.33 和 578 nM[1]。
CFT-2718 (10 nM；2-24 h) 能有效诱导 H69、H446 和 PNX-017 细胞凋亡 (通过 PARP 裂解来检测)，而在 PNX-001 胰腺细胞中无活性[1]。
CFT-2718 (10 nM；2-24 h) 可在 H69 和 H446 小细胞肺癌 (SCLC) 细胞中诱导快速且持久的 BRD4 降解 (2 小时内即可检测到)，而在 PNX-001 和 PNX-017 胰腺细胞中则会诱导延迟但持久的降解 (6 小时时可检测到)[1]。
CFT-2718 (10 nM；2-24 h) 可强效且持续地抑制转录信号通路 (降低 pSer2、pSer5 及总 RPB1 水平)，并下调 H69 和 H446 小细胞肺癌 (SCLC) 细胞，以及 PNX-001 和 PNX-017 胰腺细胞中的 MYC 表达[1]。

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

CFT-2718 相关抗体:

Western Blot Analysis[1]

Cell Line: SCLC cell lines H69, H446; pancreatic cancer cell lines PNX-001, PNX-017
Concentration: 10 nM
Incubation Time: 2, 6, 12, 24 h
Result: Induced rapid BRD4 degradation in H69 and H446 SCLC cells, with significant reduction observed within 2 hours and sustained through 24 hours.
Caused marked BRD4 reduction in PNX-001 and PNX-017 pancreatic cells by 6 hours, which remained depressed through 24 hours.
Significantly reduced levels of pSer2, pSer5, and total RPB1 in all four cell lines within 6 hours, with pSer2 levels remaining strongly depressed through 24 hours.
Reduced MYC expression in all cell lines: maximal loss occurred by 2 hours in H69 and H446 SCLC cells (with sustained suppression through 24 hours) and by 6 hours in PNX-001 and PNX-017 pancreatic cells (with partial rebound of MYC levels over time).
药代动力学
(Parmacokinetics)
Species Dose Route C0 T1/2 Vdss CL AUC0-last
Mice[1] 3 mg/kg i.v. 36087 ng/mL 5.15 h 1.24 L/kg 41.8 mL/min/kg 1194 ng·h/mL
体内研究
(In Vivo)

CFT-2718 (2-3 mg/kg；静脉注射；每周 1 次；持续 3 周) 在雌性 BALB/c 裸鼠中，2 mg/kg 剂量耐受性良好，未出现显著体重下降，但 3 mg/kg 剂量会导致 9-17%的体重下降[1]。
CFT-2718 (1-1.8 mg/kg；眼眶后注射；每周 1 次；持续 2 周) 在 B17 重症联合免疫缺陷小鼠中具有良好的耐受性，可使肝脏中 BRD4 的表达水平出现统计学意义的降低，且不会诱导显著的 caspase-3 介导的细胞凋亡[1]。
CFT-2718 (1.8 mg/kg；静脉注射；每周 1 次；持续 3 周) 在抑制 RS4;11 急性淋巴细胞白血病异种移植小鼠中可诱导肿瘤消退[1]。
CFT-2718 (1.8 mg/kg；眼眶后注射；每周 1 次；持续 3 周) 在抑制 LX-36 小细胞肺癌 PDX 肿瘤生长方面的效果显著优于对照药物，并可在肿瘤组织中诱导显著的 BRD4 降解[1]。
CFT-2718 (1.8 mg/kg；眼眶后注射；每周 1 次；持续 3 周) 可抑制 PNX-001 和 PNX-017 胰腺癌 PDX 模型的肿瘤生长，诱导肿瘤组织中 BRD4 显著降解，并导致短暂、轻度的体重下降[1]。

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

Animal Model: C.B17 scid with PNX-001 and PNX-017 pancreatic cancer cells[1]
Dosage: 1.8 mg/kg
Administration: Retro-orbital injection; once weekly; 3 weeks
Result: Inhibited PNX-001 and PNX-017 tumor growth at endpoint stage compared with vehicle.
Induced a statistically significant reduction in BRD4 H-score in excised tumor tissue compared with vehicle.
Caused a statistically significant reduction in body weight compared with vehicle and control agent groups, though this did not exceed 10% at any point.
分子量

811.37

Formula

C45H47ClN10O3
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

CFT-2718 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:

CFT-2718CFT2718CFT 2718PROTACsEpigenetic Reader Domainc-MycApoptosisMycsmall-cell lung cancerBRD4293T cellsCRBNMYCLX-36pancreatic cancerRPB1MOLT4 CRBN?/? cellsPNX-001Inhibitorinhibitorinhibit

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