2. MBM-55

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.

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MBM-55 Chemical Structure

MBM-55 Chemical Structure

CAS No. : 2083622-09-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 417 In-stock
Solution
10 mM * 1 mL in DMSO USD 417 In-stock
Solid
1 mg USD 228 In-stock
5 mg USD 380 In-stock
10 mg USD 550 In-stock
25 mg USD 840 In-stock
50 mg USD 1100 In-stock
100 mg USD 1500 In-stock
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Other Forms of MBM-55:

MBM-55 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 1 nM (Nek2), 5.4 nM (RSK1), 6.5 nM (DYRK1a), 57 nM (CHK1), 91 nM (GSK-3β), 20 nM (ABL), 370 nM (CDK2), 441nM (CDK4), 608 nM (AKT1), 5300 nM (Aurora A)[1]
In Vitro

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

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

MBM-55 Related Antibodies

Cell Cycle Analysis[1]

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[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Caused cell apoptosis in a concentration-dependent manner.
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[1].
MBM-55 (1.0 mg/kg; i.v.) treatment shows the CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.

MedChemExpress (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: Significantly suppressed tumor growth.
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 were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.
Molecular Weight

498.55

Formula

C28H27FN6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(C(C=C1)=C(OCC2=CC=CC(F)=C2)C=C1C3=CN=C4N3C=CC(C5=CN(CCN(C)C)N=C5)=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (250.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.94%

COA (249 KB) HNMR (288 KB) LCMS (270 KB)

Handling Instructions (2659 KB)

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0058 mL 10.0291 mL 20.0582 mL 50.1454 mL
5 mM 0.4012 mL 2.0058 mL 4.0116 mL 10.0291 mL
10 mM 0.2006 mL 1.0029 mL 2.0058 mL 5.0145 mL
15 mM 0.1337 mL 0.6686 mL 1.3372 mL 3.3430 mL
20 mM 0.1003 mL 0.5015 mL 1.0029 mL 2.5073 mL
25 mM 0.0802 mL 0.4012 mL 0.8023 mL 2.0058 mL
30 mM 0.0669 mL 0.3343 mL 0.6686 mL 1.6715 mL
40 mM 0.0501 mL 0.2507 mL 0.5015 mL 1.2536 mL
50 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0029 mL
60 mM 0.0334 mL 0.1672 mL 0.3343 mL 0.8358 mL
80 mM 0.0251 mL 0.1254 mL 0.2507 mL 0.6268 mL
100 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.5015 mL
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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:

MBM-552083622-09-5MBM55MBM 55Inhibitorinhibitorinhibit

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