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  3. MBM-17S

MBM-17S 

目录号: HY-101030A
产品使用指南

MBM-17S 是有效的 NIMA-related kinase 2 (Nek2) 抑制剂,IC50 值为 3 nM,通过诱导细胞周期停滞和凋亡 (apoptosis),抑制癌细胞的增殖,具有抗肿瘤活性,且对小鼠没有明显的毒性。

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MBM-17S Chemical Structure

MBM-17S Chemical Structure

CAS No. : 2083621-91-2

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  • 生物活性

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生物活性

MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice[1].

IC50 & Target

IC50: 3 nM (Nek2), 5800 nM (Aurora A)[1]

体外研究
(In Vitro)

MBM-17S inhibits MGC-803, HCT-116, and Bel-7402 cells proliferation with IC50s of 0.48, 1.06, and 4.53 μM, respectively[1].
MBM-17S (0.25-1.0 μM; 24 hours) induced G2/M phase arrest and accumulation of cells with >4N content[1].
MBM-17S (0.5-1.0 μM; 24 hours) triggers apoptosis of cancer cells[1].

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

Cell Cycle Analysis[1]

Cell Line: HCT-116 and MGC-803 cells
Concentration: 0.25-1.0 μM
Incubation Time: 24 hours
Result: Obvious accumulation of cells in the G2/M phase with >4 N DNA content.

Apoptosis Analysis[1]

Cell Line: HCT-116 and MGC-803 cells
Concentration: 0.5 μM, 1.0 μM
Incubation Time: 24 hours
Result: For HCT-116 cells, the percentage of total apoptotic cells was 39.3%±3.8% and 47.1%±0.6% at 0.5 μM and 1.0 μM, respectively. For MGC-803 cells, the percentage of total apoptotic cells increased to 32.9%±4.6% and 41.1%±0.2% at 0.25 μM and 0.5 μM, respectively.
体内研究
(In Vivo)

MBM-17S (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule[1].
MBM-17S (1.0 mg/kg; i.v.) treatment shows CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively[1].

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

Animal Model: Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts)[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; twice a day for 21 days
Result: Tmor growth was significantly suppressed.
Animal Model: Male Sprague Dawley (SD) rats[1]
Dosage: 1.0 mg/kg
Administration: IV injection (Pharmacokinetic Analysis)
Result: The CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively.
分子量

716.74

Formula

C36H40N6O10

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.

参考文献
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  • 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

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