2. Epigenetics
  3. Histone Methyltransferase
  4. AMG-193

AMG 193 是一种具有口服活性的 MTA-cooperative PRMT5 抑制剂，具有抗肿瘤活性。AMG 193 在与 MTA 复合时，通过抑制 PRMT5 优先抑制 MTAP 缺失肿瘤细胞的生长 (IC50=0.107 μM)，从而保护 MTAP 野生型的正常细胞。

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AMG-193 Chemical Structure

AMG-193 Chemical Structure

CAS No. : 2790567-82-5

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AMG-193 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP[1][2].

体外研究
(In Vitro)

AMG 193 (200 μM; 6 d) 诱导 MTAP 缺失的 HCT116 细胞的选择性剪接缺陷、细胞周期阻滞和 DNA 损伤反应[2]。

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

AMG-193 相关抗体:

Cell Cycle Analysis[2]

Cell Line: MTAP-deficient HCT116 cells
Concentration: 200 µM
Incubation Time: 6 d
Result: Reduced the S phase and increased the G2/M cell population in mtap-deficient cells.
体内研究
(In Vivo)

AMG 193 (3-100 mg/kg；p.o.；每 5 天给药一次，共给药 4 次) 在 MTAP 缺失的异种移小鼠中剂量依赖性抑制肿瘤生长[2]。
AMG 193 (100 mg/kg；p.o.；每日 1 次，持续 11 天) 使植入 DLBCL (DOHH-2) 肿瘤的小鼠体重略有下降，并使 70% 的小鼠体内肿瘤消退，并保留正常造血细胞系[2]。

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

Animal Model: HCT116 MTAP-deficient mice[2]
Dosage: 3、10、30、100 mg/kg
Administration: p.o.; The drug was administered on day 20 after mice were implanted with DLBCL (DOHH-2) tumor cells and was administered once every 5 days for a total of 4 doses.
Result: Inhibited SDMA signaling in mtap-deleted tumors at all doses.
Animal Model: Mice implanted with DLBCL (DOHH-2) tumors[2]
Dosage: 100 mg/kg
Administration: p.o.; Once daily for 11 days
Result: Caused a significant increase in the Sub-G1 population and induced tumor cell death.
分子量

444.41

Formula

C22H19F3N4O3
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 99.36%

COA (291 KB) HNMR (143 KB) RP-HPLC (233 KB) LCMS (227 KB)

产品使用指南 (1538 KB)
参考文献

AMG-193 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:

AMG-1932790567-82-5AMG193AMG 193Histone MethyltransferasePRMT5 InhibitorHCT116Inhibitorinhibitorinhibit

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产品名称：
AMG-193
目录号：
HY-153390
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