Cat. No.: HY-156437

NBI-961

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NBI-961 is a NEK2 catalytic inhibitor with human NEK2 IC₅₀ ~12-fold lower than FLT3. NBI-961 induces proteasomal degradation of NEK2. NBI-961 induces G2/mitosis arrest, apoptosis, and compromises viability in DLBCL cells and patient-derived cells. NBI-961 sensitizes DLBCL cells to doxorubicin and vincristine, and suppresses DLBCL tumor growth in mice. NBI-961 can be used for the research of diffuse large b cell lymphoma.

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Pureté: 99.73%
CAS No.: 2225902-98-5
Formule: C₂₈H₂₇F₃N₆O₂S
Masse moléculaire:568.61

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

NBI-961 Chemical Structure

CAS No.: 2225902-98-5

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

NEK2

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Cellular Effect

Cell Line	Type	Value	Description	References
MGC-803	IC₅₀	0.17 μM Compound: 17a	Antitumor activity against human MGC-803 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antitumor activity against human MGC-803 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 32992252]

In Vitro

Compared with the other 96 tested human kinases, NBI-961 exhibits high binding selectivity for NEK2, with only weak binding to FLT3 at 15 nM^[1].
NBI-961 (0.001-40 μM; 96 h) potently reduces the viability of DLBCL cell lines in vitro, with a nanomolar GI₅₀ value, and exhibits a 4.2-fold therapeutic window relative to EBV-immortalized benign peripheral B cells^[1].
NBI-961 (25-240 nM; 24-96 h) induces G₂/M cell cycle arrest in sensitive DLBCL cell lines SUDHL5 and RIVA at 24 h^[1].
NBI-961 (25-240 nM; 24-96 h) induces time- and concentration-dependent apoptosis in DLBCL cell lines^[1].
NBI-961 (19 nM, 38 nM, 76 nM; 24 h) exerts a dual-functional mechanism of action, which catalytically inhibits NEK2 (reducing p-NEK2 levels) and induces proteasomal degradation of total NEK2 protein in DLBCL cell lines SUDHL5, VAL, RIVA and U2932^[1].
NBI-961 (0.019-2.0 μM; 24-96 h) reduces the viability of the DLBCL cell line SUDHL5 and primary high-grade B-cell lymphoma cells^[1].
Inhibition of NEK2 induced by NBI-961 (25-240 nM; 96 h) shifts the proteome and phosphoproteome of NEK2-sensitive diffuse large B-cell lymphoma (DLBCL) cell lines SUDHL5 and RIVA toward an anti-mitotic and pro-apoptotic state, and reduces the level of phosphorylated AKT in SUDHL5 cells^[1].
NBI-961 (0-7.8 nM combined with 5 nM DOX or 0.15 nM VCR; 96 h) sensitizes the sensitive DLBCL cell lines SUDHL5, RIVA and U2932 to low concentrations of DOX (HY-15142A) and VCR (HY-N0488A) by inducing apoptosis, while it exerts no effect on low-sensitivity DLBCL cell lines or benign B cell lines^[1].

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

Cell Viability Assay^[1]

Cell Line:

DLBCL cell lines (U2932, RIVA, HT, SUDHL4, SUDHL5, SUDHL6, HBL1, VAL), benign EBV-immortalized peripheral B cell lines (GM22761, GM16113)
Concentration:

0.001-40 μM
Incubation Time:

96 h
Result:

Achieved nanomolar growth inhibitory concentrations (GI₅₀) in DLBCL cell lines, with particularly high potency in ABC-derived DLBCL cells.
Exhibited a 4.2-fold therapeutic window, calculated as the ratio of minimal toxic concentration (GI₅₀ in benign B cells) to minimal effective concentration (7.8 nM).

Cell Cycle Analysis^[1]

Cell Line:

DLBCL cell lines (SUDHL5, RIVA, VAL), benign EBV-immortalized peripheral B cell line (GM22671)
Concentration:

25 nM (RIVA); 80 nM (SUDHL5, GM22671); 240 nM (VAL)
Incubation Time:

24 h, 48 h, 72 h, 96 h
Result:

Induced stark G2/M arrest in SUDHL5 and RIVA cells as early as 24 h post-treatment, which persisted through 48 h.
Caused milder G2/M arrest in VAL cells.
Showed no detectable G2/M arrest in GM22671 benign B cells.

Apoptosis Analysis^[1]

Cell Line:

DLBCL cell lines (SUDHL5, RIVA, VAL), benign EBV-immortalized peripheral B cell line (GM22671)
Concentration:

25 nM (RIVA); 80 nM (SUDHL5, GM22671); 240 nM (VAL)
Incubation Time:

24 h, 48 h, 72 h, 96 h
Result:

Induced significant apoptotic death in SUDHL5 and RIVA cells starting at 24 h, which steadily increased through 96 h.
Caused no apoptosis in VAL cells until 48 h, requiring 3- to 9.6-fold higher concentrations than SUDHL5 and RIVA.
Induced apoptosis in GM22671 cells starting at 48 h, requiring ~3-fold higher concentration than RIVA.

Western Blot Analysis^[1]

Cell Line:

DLBCL cell lines (SUDHL5, VAL, RIVA, U2932)
Concentration:

19 nM, 38 nM, 76 nM (NBI-961); 10 nM (bortezomib, co-treatment)
Incubation Time:

24 h
Result:

Caused a concentration-dependent reduction in both p-NEK2 and total NEK2 protein levels in SUDHL5, VAL, RIVA, and U2932 cells.
Blocked NBI-961-induced loss of total NEK2 but did not prevent loss of p-NEK2 when co-treated with bortezomib.
Left NEK2 mRNA levels unchanged, confirming loss of NEK2 occurred at the protein level.

Cell Viability Assay^[1]

Cell Line:

DLBCL cell line (SUDHL5), primary patient-derived high-grade B cell lymphoma cells (ID# 36206)
Concentration:

0.019 μM, 0.038 μM, 0.076 μM, 0.5 μM, 2.0 μM (24 h incubation; SUDHL5); 0.038 μM, 0.076 μM, 0.5 μM, 1.0 μM, 2.0 μM (96 h incubation; primary cells)
Incubation Time:

24 h (SUDHL5); 96 h (primary cells)
Result:

Reduced the percentage of live cells in both SUDHL5 cells and primary patient-derived lymphoma cells.
Caused significant viability loss at 24 h in SUDHL5 and 96 h in primary cells.

Cell Viability Assay^[1]

Cell Line:

DLBCL cell lines (SUDHL5, RIVA, VAL, U2932, HT, SUDHL4, HBL1), benign EBV-immortalized peripheral B cell lines (GM22671, GM16113)
Concentration:

0 nM, 2.0 nM, 3.9 nM, 7.8 nM NBI-961 plus 5 nM DOX or 0.15 nM VCR; 7.8 nM NBI-961 plus 5 nM DOX (apoptosis analysis)
Incubation Time:

96 h
Result:

Significantly reduced cell viability in sensitive DLBCL cell lines SUDHL5, RIVA, and U2932 when co-treated with low, non-cytotoxic concentrations of DOX or VCR compared to DOX/VCR alone.
Induced increased apoptosis in SUDHL5 and RIVA cells with co-treatment.
Showed no chemosensitization or increased apoptosis in less sensitive VAL, HBL1, SUDHL4, and benign B cell lines.

In Vivo

NBI-961 (5 mg/kg; i.p.; daily; 8 weeks) delays diffuse large B-cell lymphoma growth and prolongs survival in humanized NSG-IL6 mice, with no observed toxicity^[1].

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

Animal Model:

NSG-TG(Hu-IL6) (NSG-IL6) (8-10 weeks old, randomized for sex, humanized)^[1]
Dosage:

5 mg/kg
Administration:

i.p.; daily; 8 weeks
Result:

Reduced bioluminescence signal over 7 weeks post-injection to delay disease onset.
Prolonged median mouse survival from 5.7 weeks to 6.4 weeks.
Showed no visible signs of distress, toxicity, weight loss, appetite loss, reduced activity, or fur tufting.

Chemical Information

CAS No. 2225902-98-5
Appearance Solid
Masse moléculaire 568.61
Formule C₂₈H₂₇F₃N₆O₂S
Color Light yellow to yellow
SMILES

CC(C1=C(C=CC=C1)C(F)(F)F)OC2=C(SC(C3=CN=C4C=C(C=CN34)C5=CN(CCN(C)C)N=C5)=C2)C(N)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (175.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7587 mL

8.7934 mL

17.5867 mL

5 mM

0.3517 mL

1.7587 mL

3.5173 mL

10 mM

0.1759 mL

0.8793 mL

1.7587 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (285 KB)
SDS (254 KB)
- English - EN (254 KB)
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- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. McCrury M, et al. Bifunctional Inhibitor Reveals NEK2 as a Therapeutic Target and Regulator of Oncogenic Pathways in Lymphoma. Molecular cancer therapeutics. 2024 Mar 04;23(3):316-329. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.7587 mL	8.7934 mL	17.5867 mL	43.9669 mL
	5 mM	0.3517 mL	1.7587 mL	3.5173 mL	8.7934 mL
	10 mM	0.1759 mL	0.8793 mL	1.7587 mL	4.3967 mL
	15 mM	0.1172 mL	0.5862 mL	1.1724 mL	2.9311 mL
	20 mM	0.0879 mL	0.4397 mL	0.8793 mL	2.1983 mL
	25 mM	0.0703 mL	0.3517 mL	0.7035 mL	1.7587 mL
	30 mM	0.0586 mL	0.2931 mL	0.5862 mL	1.4656 mL
	40 mM	0.0440 mL	0.2198 mL	0.4397 mL	1.0992 mL
	50 mM	0.0352 mL	0.1759 mL	0.3517 mL	0.8793 mL
	60 mM	0.0293 mL	0.1466 mL	0.2931 mL	0.7328 mL
	80 mM	0.0220 mL	0.1099 mL	0.2198 mL	0.5496 mL
	100 mM	0.0176 mL	0.0879 mL	0.1759 mL	0.4397 mL

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Voir tous les produits spécifiques à Isoform NEKs

Voir tous les produits spécifiques à Isoform Akt

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

NBI-961 Related Classifications

HY-156437 Related Classifications