2. Apoptosis
  3. Apoptosis c-Myc
  4. SVC112

SVC112 是一种翻译延伸 (translation elongation) 抑制剂，其通过阻止 EF2 从核糖体上的周期性解离来抑制翻译的延伸步骤。 SVC112 在多种癌细胞系 (急性髓系白血病 (AML)、多发性骨髓瘤 (Myeloma)、结直肠癌 (CRC) 和头颈部鳞状细胞癌 (HNSCC) 中显示出抑制活性。SVC112 优先阻碍 mRNA 的核糖体加工，并减少包括 Myc 和 Sox2 在内的 CSC 相关蛋白。SVC112 在血液癌细胞系中诱导凋亡 (apoptosis)，而在结直肠癌细胞系中，c-Myc 的磷酸化与其对 SVC112 的敏感性相关。SVC112 在体外可灭活 HNSCC 干细胞，并防止小鼠 HNSCC 肿瘤异种移植模型的肿瘤再生长。SVC112 可以用于头颈部鳞状细胞癌的研究。

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SVC112

SVC112 Chemical Structure

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SVC112 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC[1][2].

体外研究
(In Vitro)

SVC112 (0-10 μM, 72 h) 在多种癌细胞系中显示出广谱的生长抑制效果：急性髓系白血病 (AML-BDL-1、MV-4-11、HL-60 和 MOLM-13 细胞) (IC50 < 0.1 μM)、(THP-1、NOMO-1、MONO-MAC-6和U-937细胞) (IC50 = 0.1-0.5 μM)、(Kasumi-3 和 KG-1a 细胞) (IC50 > 1 μM)；多发性骨髓瘤 (NCI-H929、L-363、RPMI-8226、OPM-2、U266、MM.15 和 MM.1R 细胞) (IC50 < 0.1 μM)、(LP-1 细胞) (IC50 = 0.1-0.5 μM)；结直肠癌 (SW48、RKO、HCT116、WiDr 和 CL-34 细胞) (IC50 < 0.1 μM)、(HT29、MDST8、COLO201、GP2D、NCI-H747、SNU70、SW837 和 SW403 细胞) (IC50 = 0.1-0.5 μM)、(DLD-1、T84、KM-12C、SW948、Q-11、HCT-15 和 SW48 细胞) (IC50 > 1 μM)；头颈部鳞状细胞癌 (FaDu细胞) (IC50 < 0.1 μM)[1]。
SVC112 (1 μM, 2 h) 抑制 MV-4-11、NCI-H929、HCT116、FaDu、DLD-1 和 SW948 细胞的新蛋白合成[1]。
SVC112 (1 μM, 6-24 h) 在 AML 和 骨髓瘤细胞系 (AML-EOL-1、MV-4-11、OCI-AML-3、NCI-H929、RPMI-8226 和 U226B1 细胞) 中诱导凋亡，但在结直肠癌和头颈鳞癌细胞系 (HCT116 和 FaDu 细胞) 中无此作用[1]。
SVC112 (1 μM, 6 h) 在结直肠癌细胞系 (DLD-1 和 SW948 细胞) 中表现出与 c-Myc 状态相关的差异敏感性[1]。
SVC112 (0.2-0.4 μM) 与 Ulixertinib (HY-15816) (1 μM) 联用可增强生长抑制效果[1]。
SVC112 (5-1000 nM, 2 h) 在 Det562 和 FaDu 头颈鳞癌细胞中抑制蛋白合成和增殖，并增强放疗效果[2]。
SVC112 (0.1-1000 nM) 可抑制兔网织红细胞裂解物系统中无帽荧光素酶mRNA的体外非帽依赖性翻译 (IC50 = 81 nM)[2]。
SVC112 (1-10000 nM) 对 036C、067C、049C和 013C 细胞显示出抗增殖作用，IC50 值分别为 3.8 nM、9.3 nM、24.1 nM 和 50.5 nM[2]。
SVC112 (10-1000 nM, 10天) 使 013C、036C、049C 和 067C 头颈鳞癌细胞的球体形成减少[2]。
SVC112 (100 nM, 0-24 h) 通过影响翻译 (而非转录) 来消耗蛋白质，且在头颈鳞癌细胞 (013C、 036C、049C、067C) 中比在自体非癌细胞中更有效地抑制翻译[2]。
SVC112 (100-1000 nM, 6-48 h) 诱导可逆的蛋白质消耗，同时对癌症干细胞特性产生更持久的影响[2]。
SVC112 (100-1000 nM, 24 h) 在 013C、036C、067C 和 049C 细胞中显示出抗球体形成作用，该作用可通过外源性 Sox2 表达来挽救[2]。
SVC112 (100 nM, 12-24 h) 通过延迟 DNA 修复来增强 013C、036C、067C 和 049C 细胞的放疗效果[2]。

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

SVC112 相关抗体:

Apoptosis Analysis[1]

Cell Line: MV-4-11, NCI-H929, HCT116 and FaDu cells
Concentration: 1 μM
Incubation Time: 6 h
Result: Induced robust apoptosis in MV-4-11and NCI-H929 cells, but not in HCT116 and FaDu cells.

Western Blot Analysis[1]

Cell Line: AML-EOL-1, MV-4-11, MOLM-13, OCI-AML-3, NCI-H929, RPMI-8226, U226B1, THP-1, NOMO-1, Kasumi-3, HCT116 and FaDu cells
Concentration: 1 μM
Incubation Time: 6, 24 h
Result: Induced PARP cleavage concomitantly with depletion of MCL-1 and c-Myc in AML and Myeloma cell lines (AML-EOL-1, MV-4-11, OCI-AML-3, NCI-H929, RPMI-8226 and U226B1 cells), but not in CRC and HNSCC cell lines (HCT116 and FaDu cells).
Showed little sign of PARP cleavage despite loss of the unstable proteins MCL-1 and c-Myc.

Apoptosis Analysis[2]

Cell Line: Det562 and FaDu HNSCC cells
Concentration: 5, 20, 50, 100, 200, 500, 1000 nM
Incubation Time: 2 h
Result: Depleted Myc and Cyclin D1 in Det562 and FaDu HNSCC cells.
体内研究
(In Vivo)

SVC112 (60 mg/kg，腹腔注射，每日一次，持续 3 周) 在小鼠 MV-4-11、AML-EOL-1 和 HCT116 细胞移植瘤模型中显示出疗效 [1]。
SVC112 (15 mg/kg，腹腔注射，每日一次，持续 3 周) 与 Ulixertinib (HY-15816) 联合使用时，可抑制小鼠 DLD1 细胞移植瘤的肿瘤生长[1]。
SVC112 (60 mg/kg，腹腔注射，每周四次，持续 28 天) 在 CUHN036、CUHN047、CUHN004 和 CUHN013 PDX 模型中单药或联合放疗均表现出显著的肿瘤生长抑制作用[2]。

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

Animal Model: 107 MV-4-11 cells per mouse mixed 1:1 with Matrigel Matrix in 100 µL total volume were inoculated by subcutaneous injection into the right hind flank of BALB/c nude mice (6-8 weeks old females); 5 × 106 MV-4-11 cells per mouse in 100 µL PBS were inoculated into the tail vein of NOG mice (6-8 weeks old females); 1 × 106 AML-EOL-1, MV-4-11 or 5×105 HCT116 cells per mouse mixed 1:1 with Matrigel in 100 µL total volume were inoculated by subcutaneous injection into the right hind flank of nu/nu mice (5-8 weeks old females)[1]
Dosage: 60 mg/kg with QDX5 (i.p. five times weekly)
Administration: i.p., once daily for 3 weeks
Result: Showed significant tumor growth control in all three models.
Provided significant survival benefit in mice bearing MV-4-11 and AML-EOL-1 xenografts.
Showed no significant changes in body weight.
Animal Model: 1 × 106 DLD-1 cells per mouse mixed 1:1 with Matrigel in 100 µL total volume were inoculated by subcutaneous injection into the right hind flank of nu/nu mice (5-8 weeks old females)[1]
Dosage: 15 mg/kg combined with Ulixertinib (50 mg/kg)
Administration: i.p., once daily for 3 weeks
Result: Reduced tumor growth significantly compared to vehicle controls when combined with Ulixertinib whereas the single drug treatments had no significant effects.
Animal Model: Tumor pieces were implanted on both flanks of 6 to 10-week-old female Athymic Nude-Foxn1nu mice[2]
Dosage: 60 mg/kg or combined with radiation (3Gy)
Administration: i.p. twice weekly for 28 days
Result: Suppressed growth in CUHN036 (T/C = 0.45) and CUHN047 (T/C = 0.37) alone.
Inhibited growth in CUHN047 (T/C = −0.02), CUHN036 (T/C = 0.08), and CUHN004 (T/C = 0.19) when combined with radiation.
Increased inhibition of FaDu xenografts when combined with radiation (2Gy twice weekly) and Cisplatin (HY-17394) (1mg/kg weekly).
Suppressed Myc in CUHN036 and combination treatment suppressed Myc in CUHN036 and CUHN047 tumors.
Decreased CSC number.
分子量

835.74

Formula

C40H47BrN6O9
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

SVC112 相关分类

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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:

SVC112SVC 112SVC-112Apoptosisc-MycMycAcute Myeloid Leukemia (AML)Multiple Myeloma (Myeloma)Colorectal Cancer (CRC)and Head and Neck Squamous Cell Carcinoma (HNSCC)cancerInhibitorinhibitorinhibit

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