2. Apoptosis Cell Cycle/DNA Damage Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. c-Myc Early 2 Factor (E2F) TNF Receptor MDM-2/p53 Reactive Oxygen Species (ROS) Apoptosis
  4. JR4-187

JR4-187 是一种具有口服活性的铜依赖性的抗癌剂。JR4-187 可下调癌细胞中参与氧化磷酸化、MYC 靶标及 E2F 靶标的基因，同时上调参与 TNF-α 信号通路、p53 通路及 KRAS 信号通路的基因，下调 CTR1 蛋白。JR4-187 可诱导 ROS 产生、细胞凋亡 (apoptosis)、铜依赖性细胞毒性，同时对 KRAS 突变型癌细胞具有选择性细胞毒性。JR4-187 在胰腺癌小鼠模型中具有良好的耐受性。JR4-187 可用于胰腺导管腺癌、结肠癌、直肠癌等癌症的相关研究。

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JR4-187

JR4-187 Chemical Structure

CAS No. : 2446965-01-9

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JR4-187 相关抗体

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查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JR4-187 is an orally active, copper-dependent anticancer agent. JR4-187 downregulates genes involved in oxidative phosphorylation, MYC targets and E2F targets in cancer cells, while upregulates genes involved in the TNF-α signaling pathway, p53 pathway and KRAS signaling pathway, and downregulates CTR1 protein. JR4-187 induces ROS production, apoptosis, copper-dependent cytotoxicity, and exhibits selective cytotoxicity against KRAS-mutant cancer cells. JR4-187 is well tolerated in mouse models of pancreatic cancer. JR4-187 can be used in research related to cancers such as pancreatic ductal adenocarcinoma, colon cancer and rectal cancer[1][2].

体外研究
(In Vitro)

JR4-187 (2 μM; 24 h) 可下调 HCT116 细胞中参与氧化磷酸化、MYC 靶标及 E2F 靶标的基因，同时上调参与 TNF-α 信号通路、p53 通路及 KRAS 信号通路的基因[1]。
JR4-187 (2.5-15 μM; 4-24 h) 可显著下调 HCT116、MIA PaCa-2、PANC1 和 BXPC3 细胞中 MYC、NDUFS7 蛋白的表达[1]。
JR4-187 (0.03-1 μM; 6 days) 与特定化合物联用时，在 HCT116 结肠癌细胞中可产生细胞毒性协同作用 (与 Danazol (HY-B1029)、Metformin (HY-B0627)、IACS-010759 (HY-112037)、Rotenone (HY-B1756)、DX2-201 (HY-145303)、DX3-213B (HY-144310)、AGB-374 联用)、拮抗作用 (与 MYCi361 (HY-129600)、10058-F4 (HY-12702)、MYCMI-6 (HY-124675) 联用)[1]。
JR4-187 (10 μM; 24 h) 可显著下调 HCT116 和 MIA PaCa-2 细胞中 CTR1 蛋白的表达[1]。
JR4-187 (2.5 μM; 24 h) 与 5 μM AGB-374 (HY-182242) 联合作用可在 HCT116 结肠癌细胞中协同下调 MYC 和 NDUFS7 的蛋白表达[1]。
JR4-187 (Compound 39) 可强效抑制 KRAS 突变型胰腺癌和结肠癌细胞的增殖，在 SU.86.86 细胞 (IC50 = 0.8 μM) 和 MIA PaCa-2 细胞 (IC50 = 1.9 μM) 中活性最高，在 KRAS 野生型 BxPC-3 细胞中活性较低[2]。
JR4-187 (0-10 μM; 6 days) 具有铜依赖性细胞毒性，在 MIA PaCa-2 和 HCT116 细胞中与 CuSO4 表现出强协同作用，且在铜螯合剂 TTM (HY-128530 ) 存在下活性降低[2]。
JR4-187 (0-5 μM; 6 days) 与 COX2 抑制剂 Celecoxib (HY-14398) 和 Rofecoxib (HY-17372) 在抑制 HCT116、MIA PaCa-2 和 BxPC-3 细胞的集落形成方面表现出强协同作用[2]。
JR4-187 (0-1 μM; 6 days) 在 HCT116 和 MIA PaCa-2 细胞中可诱导 ROS 依赖性细胞死亡[2]。
JR4-187 (0-10 μM; 1-6 days) 可通过细胞凋亡和坏死性凋亡部分诱导 MIA PaCa-2 和 HCT116 细胞死亡[2]。

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

JR4-187 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT116 human colon cancer cells
Concentration: 10 μM
Incubation Time: 4 h; 24 h
Result: Significantly downregulated MYC protein levels relative to control cells.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 and BXPC3 human pancreatic cancer cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Decreased MYC protein abundance in both MIA PaCa-2 and BXPC3 cells.

Western Blot Analysis[1]

Cell Line: HCT116 human colon cancer cells, MIA PaCa-2 and PANC1 human pancreatic cancer cells
Concentration: 2.5, 5, 7.5, 10, 15 μM
Incubation Time: 24 h
Result: Caused a dose-dependent reduction in MYC protein levels in HCT116, MIA PaCa-2, and PANC1 cells.\nCaused a dose-dependent reduction in NDUFS7 protein levels in HCT116, MIA PaCa-2, and PANC1 cells.

Cell Cytotoxicity Assay[1]

Cell Line: HCT116 human colon cancer cells
Concentration: 0.03, 0.1, 0.3, 1 μM
Incubation Time: 6 days
Result: Showed strong cytotoxic synergy with Danazol.
Showed strong antagonism with MYCi361, 10058-F4, and MYCMI-6.
Showed no significant interaction with 10074-G5.
Showed significant synergy with metformin, IACS-010759, and Rotenone.
Showed weak synergy with 2-DG.
Showed significant synergy with DX2-201, DX3-213B, and AGB-374.

Western Blot Analysis[1]

Cell Line: HCT116 human colon cancer cells and MIA PaCa-2 human pancreatic cancer cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Caused a marked decrease in CTR1 protein levels in both HCT116 and MIA PaCa-2 cells, with a log10 fold change of ~-0.3 in HCT116 cells and ~-0.15 in MIA PaCa-2 cells.

Western Blot Analysis[1]

Cell Line: HCT116 human colon cancer cells
Concentration: 2.5 μM (alone and in combination with 5 μM AGB-374)
Incubation Time: 24 h
Result: Led to synergistic downregulation of both MYC and NDUFS7 protein levels in HCT116 cells, compared to monotherapy with either agent.

Cell Cytotoxicity Assay[2]

Cell Line: MIA PaCa-2, HCT116
Concentration: 0, 0.018, 0.05, 0.16, 0.5 μM/0, 0.03, 0.1, 0.3, 1 μM/0. 0.3. 1.1, 3.3, 10 μM
Incubation Time: 6 days
Result: Showed strong synergy with copper sulfate (CuSO4) in both cell lines, as measured by the HSA model in Combenefit software.
Exhibited significantly reduced cytotoxic activity when combined with copper chelator ammonium Tetrathiomolybdate (TTM).

Cell Proliferation Assay[2]

Cell Line: HCT116, MIA PaCa-2, BxPC-3
Concentration: 0, 0.03, 0.1, 0.3, 1 μM (HCT116 with Celecoxib); 0, 0.018, 0.05, 0.16, 0.5 μM (MIA PaCa-2 with Celecoxib; MIA PaCa-2 with Rotecoxib); 0, 0.03, 0.1, 0.3, 1 μM (HCT116 with Rotecoxib); 0, 0.18, 0.5, 1.6, 5 μM ( BxPC-3 with Celecoxib)
Incubation Time: 6 days
Result: Showed strong synergy with celecoxib across all three cell lines, as measured by the HSA model in Combenefit software.
Exhibited strong synergy with rotecoxib in HCT116 and MIA PaCa-2 cells, as measured by the HSA model in Combenefit software.

Cell Cytotoxicity Assay[2]

Cell Line: HCT116, MIA PaCa-2
Concentration: 0, 0.03, 0.1, 0.3, 1 μM (HCT116); 0, 0.018, 0.05, 0.16, 0.5 μM (MIA PaCa-2)
Incubation Time: 6 days
Result: Induced cell death that was rescued by pretreatment with ROS scavenger N-acetyl cysteine (NAC) in both cell lines.

Cell Cytotoxicity Assay[2]

Cell Line: MIA PaCa-2, HCT116
Concentration: 0, 0.018, 0.05, 0.16, 0.5 μM (MIA PaCa-2 with Z-VAD-FMK; MIA PaCa-2 with Necrostatin-1); 0, 0.03, 0.1, 0.3, 1 μM (HCT116 with Z-VAD-FMK); 0, 0.07, 0.2, 0.6, 2 μM (HCT116 with necrostatin-1); 10 μM (WB for apoptosis markers); 10 μM (WB for necroptosis markers)
Incubation Time: 6 days/48 h (WB for apoptosis markers); 48 h (WB for necroptosis markers)
Result: Induced cell death that was partially rescued by apoptosis inhibitor Z-VAD-FMK and necroptosis inhibitor necrostatin-1 in both cell lines.
Increased cleaved PARP, cleaved caspase-9, cleaved caspase-3 (apoptosis markers) in cells treated for 48 h, as confirmed by Western blot analysis.
Increased phospho-RIP3 (necroptosis marker) in cells treated for 1 h, as confirmed by Western blot analysis.
药代动力学
(Parmacokinetics)
Species Dose Route C0 AUC0-last AUC0-inf T1/2 CL Vss Cmax Bioavailability
Mice[2] 15 mg/kg i.v. 3458 ng/mL 6014 ng·h/mL 6087 ng·h/mL 2.8 h 37.7 mL/min/kg 7.1 L/kg / /
Mice[2] 30 mg/kg p.o. / 6639 ng·h/mL 6801 ng·h/mL 4.9 h / / 1017 ng/mL 55.2 %
体内研究
(In Vivo)

JR4-187 (20-40 mg/kg；腹腔注射；每日；第 1-28 天) 在携带有 PAN02 胰腺癌同系异体移植物的雌性 C57BL/6 小鼠中具有良好的耐受性[2]。

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

Animal Model: C57BL/6 (female)[2]
Dosage: 40 mg/kg (days 1-20); 20 mg/kg (days 21-28)
Administration: i.p.; daily; days 1-28
Result: Showed no significant loss in body weight.
分子量

436.48

Formula

C23H25FN6O2
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

JR4-187 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:

JR4-1872446965-01-9c-MycEarly 2 Factor (E2F)TNF ReceptorMDM-2/p53Reactive Oxygen Species (ROS)ApoptosisMycTumor Necrosis Factor ReceptorTNFRCD-1 miceanticancer agentHCT116 cellsPDAC syngeneic mouse modelsKRAS-mutant cancer cellsPDAC allograft mouse modelspancreatic ductal adenocarcinomacolon cancer and rectal cancerC57BL/6miceInhibitorinhibitorinhibit

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