2. CXJ2080

CXJ2080 是一种选择性的基于 PROTAC 的 CDK7 降解剂。CXJ2080 招募 VHL E3 连接酶，诱导依赖泛素-蛋白酶体途径的 CDK7 降解，破坏 CDK7-cyclin H-MAT1 复合物，抑制 CDK7 依赖的 RNA 聚合酶 II CTD Ser5、CDK1 Thr161 及 CDK2 Thr160 磷酸化。CXJ2080 激活 p53-p21 轴，抑制 MYC 驱动的信号通路，诱导白血病细胞周期阻滞、凋亡 (apoptosis) 和分化，降低 CD117 表达，对血小板和正常 PBMC 无损伤，在洗脱后可维持 CDK7 持续降解。CXJ2080 可用于急性白血病的研究。
(粉色: Ligands for Target Protein for PROTAC 配体 (HY-183071)；蓝色: Ligands for E3 Ligase 和 VHL 配体 (HY-170348)；黑色: 连接子)。

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CXJ2080

CXJ2080 Chemical Structure

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CXJ2080 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

CXJ2080 is a selective PROTAC-based CDK7 degrader. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia[1]. (Pink: Ligands for Target Protein for PROTAC ligand (HY-183071); Blue: Ligands for E3 Ligase and VHL ligand (HY-170348); Black: linker).

体外研究
(In Vitro)

CXJ2080 (0.5-200 nM；6 小时) 可强效降解 MV4-11 急性髓系白血病细胞中的 CDK7，其 DC50 为 0.88 nM，最大降解效率>98%[1]。
CXJ2080 (72 小时) 可强效抑制 RS4;11 急性淋巴细胞白血病细胞 (IC50 = 17.29 nM) 和 MV4-11 急性髓系白血病细胞的增殖 (IC50 = 4.31 nM)[1]。
CXJ2080 (72 小时) 可抑制原代急性髓系白血病患者来源细胞样本的增殖[1]。
CXJ2080 (100 nM；4 小时预处理) 可在 MV4-11 急性髓系白血病细胞中诱导 CDK7 持续降解，且洗脱后抑制作用可维持 48 h[1]。
CXJ2080 (5-100 nM；8 小时) 可在 MV4-11 急性髓系白血病细胞中诱导剂量依赖性的 CDK7 降解、p53 积累、Myc 下调以及 p21 蛋白的双相应答[1]。
CXJ2080 (5-100 nM；12 小时) 可在 MV4-11 急性髓系白血病细胞中诱导剂量依赖性细胞周期阻滞，且在较高浓度下会增加 SubG1 期细胞的累积[1]。
CXJ2080 (5-100 nM；48 小时) 可在 MV4-11 急性髓系白血病细胞中诱导剂量依赖性凋亡[1]。
CXJ2080 (5-100 nM；24 小时) 可显著降低 MV4-11 急性髓系白血病细胞中 CD117 (c-KIT) 干性标志物的表达[1]。

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

CXJ2080 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 100 nM
Incubation Time: 4 h
Result: Maintained CDK7 degradation for 48 h post-washout.

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 5 nM; 20 nM; 100 nM
Incubation Time: 8 h
Result: Degraded CDK7 in a dose-dependent manner.
Induced accumulation of p53 protein.
Downregulated Myc protein.
Caused a biphasic response in p21 protein levels (upregulated at low concentrations, downregulated at high concentrations).

Cell Cycle Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 5 nM; 20 nM; 100 nM
Incubation Time: 12 h
Result: Induced cell cycle arrest in a dose-dependent manner.
Increased accumulation of cells in the SubG1 phase at higher concentrations.

Apoptosis Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia cells
Concentration: 5 nM; 20 nM; 100 nM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner.
Showed a higher proportion of apoptotic cells observed at higher concentrations.
Exhibited more potent apoptotic effects than TZ1104.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t F T1/2
Mice[1] 10 mg/kg i.p. 1014 ng·h/mL 81.6 % /
Mice[1] 10 mg/kg i.v. / / 2.5 h
Mice[1] 10 mg/kg i.v. / / 2.5 h
体内研究
(In Vivo)

CXJ2080 (20-50 mg/kg；静脉注射；隔日一次；2 周) 以 50 mg/kg 隔日一次静脉注射给药时，可在 RS4;11 异种移植肿瘤中实现强效肿瘤生长抑制及选择性 CDK7 降解，同时对 PBMCs 无损伤[1]。
CXJ2080 (20-50 mg/kg；静脉注射；每隔 1 天；3 周) 以 50 mg/kg 的剂量每隔 1 天静脉注射给药时，可在 MV4-11 异种移植肿瘤中实现强效的肿瘤生长抑制，并选择性降解 CDK7，同时不损伤外周血单个核细胞 (PBMCs) 且维持正常的血小板参数[1]。
CXJ2080 (20 mg/kg；静脉注射；隔日一次；共 21 天) 以 20 mg/kg 的剂量隔日静脉注射给药，可显著提高播散性 Molm13 急性髓系白血病小鼠的存活率[1]。

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

Animal Model: Nu/Nu (female; 6-8 weeks old; implanted subcutaneously in
the right flank with 5 × 106 RS4;11 cells for a RS4;11 subcutaneous xenograft model)[1]
Dosage: 20 mg/kg; 50 mg/kg
Administration: i.v.; every other day; 2 weeks
Result: Resulted in tumor weights similar to vehicle controls at 20 mg/kg.
Significantly reduced tumor weights relative to vehicle controls at 50 mg/kg.
Achieved robust CDK7 degradation in tumor tissues at 50 mg/kg.
Caused no significant reduction in CDK7 levels in PBMCs at 50 mg/kg.
Animal Model: Nu/Nu (female; 6-8 weeks old; implanted subcutaneously in
the right flank with 5 × 106 MV4-11cells for a MV4-11 subcutaneous xenograft model)[1]
Dosage: 20 mg/kg; 50 mg/kg
Administration: i.v.; every other day; 3 weeks
Result: Resulted in tumor weights similar to vehicle controls at 20 mg/kg.
Significantly reduced tumor weights relative to vehicle controls at 50 mg/kg.
Achieved robust CDK7 degradation in tumor tissues at 50 mg/kg.
Caused no significant reduction in CDK7 levels in PBMCs at 50 mg/kg.
Maintained stable platelet counts, platelet-large cell ratio (P-LCR), and plateletcrit (PCT) throughout the treatment period at 50 mg/kg.
Animal Model: NOD scid gamma (NSG) (female; 6-8 weeks old; inoculated intravenously with 2 × 104
Molm13 cells via the tail vein for a Molm13 disseminated xenograft model)[1]
Dosage: 20 mg/kg
Administration: i.v.; every other day; 21 days
Result: Significantly extended the survival of Molm13 tumor-bearing mice relative to vehicle controls.
Maintained a low leukemia burden in spleens of two surviving mice at the experimental endpoint.
分子量

1030.74

Formula

C51H68ClN11O6S2
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

CXJ2080 相关分类

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  • 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:

CXJ2080CXJ 2080CXJ-2080RS4;11 acute lymphoblastic leukemia cellsRNA polymerase II CTD Ser5p53-p21 axisubiquitin-proteasomeCDK2 Thr160MV4-11 acute myeloid leukemia cellsVHL E3 ligaseCDK1 Thr161MYCCDK7Inhibitorinhibitorinhibit

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