MBM-17

Cat. No.: HY-101030: FAQs
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MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 3 nM. It 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.

For research use only. We do not sell to patients.

MBM-17 Chemical Structure

CAS No. : 2083621-90-1

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•Related Small Molecules:

•Related Proteins:

View All NEKs Isoform Specific Products:

View All Isoforms

NEK1 NEK2 NEK6 NEK7

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

NEK2

3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Bel-7402	IC₅₀	4.53 μM Compound: 42c; MBM-17	Cytotoxicity against human Bel7402 cells measured after 72 hrs by MTT assay Cytotoxicity against human Bel7402 cells measured after 72 hrs by MTT assay	[PMID: 28039836]
HCT-116	IC₅₀	1.06 μM Compound: 42c; MBM-17	Cytotoxicity against human HCT116 cells measured after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells measured after 72 hrs by MTT assay	[PMID: 28039836]
MGC-803	IC₅₀	0.48 μM Compound: 42c; MBM-17	Cytotoxicity against human MGC803 cells measured after 72 hrs by MTT assay Cytotoxicity against human MGC803 cells measured after 72 hrs by MTT assay	[PMID: 28039836]

In Vitro

MBM-17 (compound 42c) inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.48, 1.06, 4.53 μM, respectively^[1].
MBM-17 (0.25-1.0 μM; 24 hours) induced G2/M phase arrest and accumulation of cells with >4N content^[1].
MBM-17 (0.5-1.0 μM; 24 hours) triggers apoptosis of cancer cells^[1].

MedChemExpress (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.

In Vivo

MBM-17 (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule^[1].
MBM-17 (1.0 mg/kg; i.v.) treatment shows CL, V_ss, T_1/2, AUC_0-t, and AUC_0-∞ 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].

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:	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, V_ss, T_1/2, AUC_0-t, and AUC_0-∞ values of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively.

Molecular Weight

480.56

Formula

C₂₈H₂₈N₆O₂

CAS No.

2083621-90-1

Appearance

Solid

Color

White to off-white

SMILES

NC(C(C=C1)=C(OCC2=CC=CC=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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Xi JB, et al. Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities. Eur J Med Chem. 2017 Jan 27;126:1083-1106. [Content Brief]

MBM-17 Related Classifications

Molarity Calculator
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The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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

MBM-172083621-90-1MBM17MBM 17NEKsApoptosisNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesantitumorselectivityNek2proliferationcellcyclearrestapoptosisInhibitorinhibitorinhibit

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