MBM-55|cas:2083622-09-5|西域试剂

MBM-55,99.17%

产品编号：Bellancom-101029| CAS NO：2083622-09-5| 分子式：C₂₈H₂₇FN₆O₂| 分子量：498.55

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-101029		￥4800.00	杭州北京（现货）
Bellancom-101029		￥8000.00	杭州北京（现货）

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MBM-55

产品介绍

MBM-55 是有效的 NIMA-related kinase 2 (Nek2) 抑制剂，IC₅₀ 值为 1 nM，是其他激酶选择性的 20 倍甚至更高，除了 RSK1 (IC₅₀=5.4 nM) 和 DYRK1a (IC₅₀=6.5 nM)。MBM-55 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。

生物活性

MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC₅₀=5.4 nM) and DYRK1a (IC₅₀=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.

体外研究

MBM-55 (compound 42g) inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC₅₀s of 0.53, 0.84, 7.13 μM, respectively.
MBM-55 (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells.
MBM-55 (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells.

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

Cell Cycle Analysis

Cell Line:	HCT-116 cells
Concentration:	0.5, 1 μM
Incubation Time:	24 hours
Result:	Induced G2/M phase arrest and accumulation of cells with >4N content.

Apoptosis Analysis

Cell Line:	HCT-116 cells
Concentration:	0.5, 1 μM
Incubation Time:	24 hours
Result:	Caused cell apoptosis in a concentration-dependent manner.

体内研究
(In Vivo)

MBM-55 (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule in nude mice bearing HCT-116 xenografts.
MBM-55 (1.0 mg/kg; i.v.) treatment shows the CL, V_ss, T_1/2, AUC_0-t, and AUC_0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.

西域 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)
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; twice a day for 21 days
Result:	Significantly suppressed tumor growth.

Animal Model:	Male Sprague Dawley (SD) rats
Dosage:	1.0 mg/kg
Administration:	IV injection (Pharmacokinetic Analysis)
Result:	The CL, V_ss, T_1/2, AUC_0-t, and AUC_0-∞ values were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.

体内研究

西域 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)
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; twice a day for 21 days
Result:	Significantly suppressed tumor growth.

Animal Model:	Male Sprague Dawley (SD) rats
Dosage:	1.0 mg/kg
Administration:	IV injection (Pharmacokinetic Analysis)
Result:	The CL, V_ss, T_1/2, AUC_0-t, and AUC_0-∞ values were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.

体内研究

西域 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)
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; twice a day for 21 days
Result:	Significantly suppressed tumor growth.

Animal Model:	Male Sprague Dawley (SD) rats
Dosage:	1.0 mg/kg
Administration:	IV injection (Pharmacokinetic Analysis)
Result:	The CL, V_ss, T_1/2, AUC_0-t, and AUC_0-∞ values were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (250.73 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0058 mL	10.0291 mL	20.0582 mL
5 mM	0.4012 mL	2.0058 mL	4.0116 mL
10 mM	0.2006 mL	1.0029 mL	2.0058 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献