2. Epigenetics Metabolic Enzyme/Protease
  3. METTL3 Cytochrome P450
  4. EP102

EP102 是一种口服有效、选择性的 METTL3/METTL14 复合物抑制剂，其 IC50 为 2 nM。EP102 可降低细胞内 N6-甲基腺苷水平、抑制癌细胞增殖，从而抑制小鼠模型中的肿瘤生长。EP102 可用于急性髓系白血病、卵巢实体瘤及晚期实体瘤的研究。

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EP102

EP102 Chemical Structure

CAS No. : 3050818-07-7

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EP102 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EP102 is an orally active, selective inhibitor of the METTL3/METTL14 complex with an IC50 of 2 nM. EP102 reduces intracellular N6-methyladenosine levels, inhibits cancer cell proliferation, and thereby suppresses tumor growth in mouse models. EP102 is applicable for the research of acute myeloid leukemia, ovarian solid tumors and advanced solid tumors[1].

IC50 & Target[1]

CYP3A4

0.9 nM (IC50)

CYP3A5

16 nM (IC50)

体外研究
(In Vitro)

EP102 可抑制 Kasumi-1、MV-4-11、Calu-6、A549、FaDu、SK-OV-3 和 Caov-3 人癌细胞系的活力，其 72 h 时的 IC50 值范围为 31 nM 至 225 nM[1]。
EP102 可降低 Kasumi-1、MV-4-11、Calu-6、A549、FaDu 及 SK-OV-3 人源癌细胞系的细胞内 m6A 水平，其 IC50 值范围为 6 nM 至 19 nM[1]。
EP102 在大鼠、小型猪和人肝微粒体中表现出代谢稳定性，半衰期分别为 149 min、44 min 和 53 min[1]。
EP102 可选择性抑制人源 CYP3A4，其 IC50 为 0.9 μM；同时可抑制人源 CYP3A5，IC50 为 16 μM，但对其他 8 种受试的主要人源 CYP 无显著抑制作用[1]。

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

EP102 相关抗体:

Real Time qPCR[1]

Cell Line: Kasumi-1, MV-4-11, Calu-6, A549, FaDu, and SK-OV-3 human cancer cell lines
Concentration: IC50
Incubation Time: /
Result: Downregulated the intracellular m6A levels in with IC50 values ranging from 6 nM to 19 nM.
体内研究
(In Vivo)

EP102 (20-47 mg/kg；口服；每日 1 次，每周 3 次；持续 4 周) 可抑制弥散性小鼠异种移植模型中的 AML 肿瘤生长，与 20 mg/kg 口服每日给药剂量相比，47 mg/kg 剂量显示出更优的效果[1]。
EP102 (47 mg/kg；口服；每周 3 次；32 天) 在卵巢癌卵巢内小鼠异种移植模型中，以 47 mg/kg 剂量每周口服给药 3 次时，可实现>90% 的肿瘤生长抑制并减少转移[1]。

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

Animal Model: NSG mice with Acute myeloid leukemia (AML) (female; disseminated xenograft model via intravenous injection of 2 × 10^6 MV-4-11-Luc-mCh-Puro cells)[1]
Dosage: 20 mg/kg; 47 mg/kg
Administration: p.o.; QD (20 mg/kg), TIW (47 mg/kg); 4 weeks
Result: Restricted AML tumor spread as shown by bioluminescence imaging with both dosing regimens.
Reduced levels of hCD45+ human AML cells in bone marrow with both dosing regimens.
Showed no depletion of mouse mCD45+ cells.
Demonstrated superior efficacy with the 47 mg/kg TIW regimen compared to the 20 mg/kg QD regimen.
Maintained stable body weights in treated mice, indicating well-tolerated treatment.
Animal Model: Balb/c mice with Ovarian cancer (female; intraovarian xenograft model via implant of SK-OV-3-Luc cells)[1]
Dosage: 47 mg/kg
Administration: p.o.; TIW; 32 days
Result: Achieved >90% tumor growth inhibition (TGI) relative to vehicle controls over the 32-day treatment period via bioluminescence measurement.
Reduced metastasis in the intestines, an effect not observed with the positive control Olaparib.
Maintained stable body weights in treated mice and showed no macroscopic adverse events, indicating well-tolerated treatment.
分子量

488.65

Formula

C27H32N6OS
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

EP102 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

EP1023050818-07-7EP 102EP-102METTL3Cytochrome P450Methyltransferase-like 3CYPsMETTL3/METTL14 complexadvanced solid tumorsN6-methyladenosineMV-4-11ovarian solid tumorsKasumi-1acute myeloid leukemiaA549FaDuCalu-6Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-183186
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