2. MAPK/ERK Pathway Cell Cycle/DNA Damage Immunology/Inflammation
  3. MNK DNA/RNA Synthesis Interleukin Related Eukaryotic Initiation Factor (eIF)
  4. ETC-501

ETC-501 是一种可穿透血脑屏障、口服有效且选择性 MNK1/MNK2 抑制剂，对 MNK1 的 IC50 为 0.033 μM，对 MNK2 的 IC50 为 0.111 μM。ETC-501 能够抑制胶质母细胞瘤细胞增殖，损伤 DNA 损伤修复功能，延缓细胞周期进程，并抑制核糖体生物发生。ETC-501 可增强 Temozolomide (HY-17364) 诱导的细胞衰老，减弱衰老相关分泌表型，同时增强细胞对 Navitoclax (HY-10087) 的敏感性。ETC-501 可用于胶质母细胞瘤的相关研究。

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ETC-501

ETC-501 Chemical Structure

CAS No. : 3094990-88-9

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ETC-501 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ETC-501 is a blood-brain barrier-permeable, orally active, and selective MNK1/MNK2 inhibitor, with an IC50 of 0.033 μM against MNK1 and 0.111 μM against MNK2. ETC-501 inhibits glioblastoma cell proliferation, impairs DNA damage repair function, delays cell cycle progression, and suppresses ribosome biogenesis. ETC-501 enhances Temozolomide (HY-17364)-induced cellular senescence, attenuates the senescence-associated secretory phenotype, and increases cellular sensitivity to Navitoclax (HY-10087). ETC-501 is applicable to research related to glioblastoma[1].

体外研究
(In Vitro)

ETC-501 (0-20 μM; 24 h) 可呈剂量依赖性地抑制 eIF4E 磷酸化，并降低 LN-229 和 T98G 胶质母细胞瘤细胞中 Cyclin D1 蛋白水平[1]。
ETC-501 (0-10 μM) 可抑制 LN-229 和 T98G 胶质母细胞瘤细胞的活力，其 GI50 值分别为 4.035 μM 和 6.122 μM，并可降低患者来源 GPCs 的肿瘤球形成能力和干细胞频率[1]。
ETC-501 (0-10 μM; 4 h) 呈剂量依赖性地损伤 LN-229、T98G 和 U-87MG 胶质母细胞瘤细胞的 DNA 合成[1]。
ETC-501 (8 h) 会损害经 Palbociclib (HY-50767) 同步化的 LN-229 和 U-87MG 胶质母细胞瘤细胞中 G1 期到 S 期的进程[1]。
ETC-501 (5-10 μM; 14 days) 可诱导 LN-229 和 U-87MG 胶质母细胞瘤细胞发生衰老[1]。
ETC-501 (5-10 μM; 10 days) 可降低关键炎性细胞因子和趋化因子 (包括 IL-6、IL-8 和 CCL2) 的水平[1]。
ETC-501 (10 μM; 6 days) 联合 TMZ (HY-17364) 可使 LN-229 胶质母细胞瘤细胞进入衰老预激状态，显著增强其对 Navitoclax (HY-10087) 诱导的细胞死亡及凋亡的敏感性[1]。

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

ETC-501 相关抗体:

Western Blot Analysis[1]

Cell Line: LN-229, T98G (human glioblastoma cell lines)
Concentration: 0, 0.1. 1, 2.5, 5, 10 and 20 μM
Incubation Time: 24 h
Result: Caused a dose-dependent reduction in phosphorylation of eIF4E without altering total eIF4E protein levels.
Reduced Cyclin D1 protein levels.
药代动力学
(Parmacokinetics)
Species Dose Route AUC T1/2
Mice[1] 10 mg/kg p.o. 4.51 h 3.84 h
体内研究
(In Vivo)

ETC-501 (100 mg/kg；口服灌胃；每日一次；21 天) 在携带原位或皮下胶质母细胞瘤的 NSG 小鼠中，与 TMZ (HY-17364) 联合使用时可增强肿瘤细胞衰老并减弱衰老相关分泌表型，再联合 Navitoclax (HY-10087) 能有效清除衰老细胞[1]。

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

Animal Model: NOD-SCID gamma (NSG, NOD.Cg-PrkdcscidIl2rgtm1wjl/SzJ) (6-8-week-old male; subcutaneous glioblastoma model)[1]
Dosage: 100 mg/kg
Administration: oral gavage; daily; 21 days
Result: Reduced excised tumor p-eIF4E levels by ~50%.
Induced senescent tumor cells (SA-β-gal positive) when combined with TMZ, with non-statistically significant trend toward higher SA-β-gal and p21 levels compared to TMZ alone.
Resulted in widespread tumor necrosis, near absence of SA-β-gal-positive cells, and markedly reduced p21 expression when combined with TMZ and navitoclax.
Animal Model: NOD-SCID gamma (NSG, NOD.Cg-PrkdcscidIl2rgtm1wjl/SzJ) (6-8-week-old male; orthotopic intracranial glioblastoma model)[1]
Dosage: 100 mg/kg
Administration: oral gavage; daily; 21 days
Result: Reduced p-eIF4E levels in contralateral and ipsilateral brain tissue by ~60%.
Did not significantly extend survival compared to vehicle control when administered alone.
Showed non-statistically significant trend toward improved survival compared to TMZ alone, and induced senescence (SA-β-gal positive) in orthotopic tumors when combined with TMZ.
Did not improve survival beyond TMZ alone when combined with TMZ and navitoclax, with residual SA-β-gal-positive senescent cells detected post-treatment.
分子量

452.51

Formula

C26H24N6O2
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

ETC-501 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:

ETC-5013094990-88-9ETC501ETC 501MNKDNA/RNA SynthesisInterleukin RelatedEukaryotic Initiation Factor (eIF)Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseILMNK2ribosome biogenesistemozolomidecell cycle regulationMNK1glioblastoma cellsDNA damage repairMYC signalinginflammationDNA replicationInhibitorinhibitorinhibit

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