Art. -Nr.: HY-157396

JAB-2485

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JAB-2485 is an orally active and selective Aurora kinase A (AURKA) inhibitor with an IC₅₀ value of 0.327 nM. JAB-2485 exhibits inhibitory activity against various tumor cell lines such as neuroblastoma, triple-negative breast cancer, small cell lung cancer, and epithelial ovarian cancer. JAB-2485 can induce cell cycle arrest and apoptosis in tumor cells. JAB-2485 has antitumor activity.

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Reinheit: 99.87%
CAS. Nr.: 2899209-55-1
Formel: C₂₅H₂₈ClF₂N₅O₂
Molecular Weight:503.97

Speicherung:

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

JAB-2485 Chemical Structure

CAS. Nr.: 2899209-55-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Aurora A

0.327 nM (IC₅₀)

Caspase 3

Caspase-7

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

In Vitro

JAB-2485 (0-2 μM; 16 h) inhibits Thr288 phosphorylation of AURKA in NCI-H446 cells (IC₅₀: 2.08 nM)^[1].
JAB-2485 (0-10 μM; 24-48 h) inhibits the viability of NCI-H446 cells by inducing cell cycle G2/M phase arrest and apoptosis (increasing Caspase 3/7 activity)^[1].

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

Western Blot Analysis^[1]

Cell Line:

NCI-H446 cells
Concentration:

0, 0.64, 3.2, 16, 80, 400 and 2000 nM
Incubation Time:

16 h
Result:

Significantly decreased the level of AURKA phosphorylation on Thr288, a marker for AURKA activation, in a dose-dependent manner.

In Vivo

JAB-2485 (10 mg/kg; p.o.; single dose) inhibits AURKA phosphorylation by 80% within 1 hour and lasts for 12 hours in NCI-H446 xenograft nude mouse models^[1].
JAB-2485 (2.5-20 mg/kg; p.o. for 32-41 days) has antitumor activity in NCI-H446, NCI-H69 and IMR-32 xenograft mouse models^[1].
Pharmacokinetic Analysis in rats and dogs^[1]

Species	Route	Dose (mg/kg)	CL (mL/min/kg)	V_ss (L/kg)	T_max (h)	T_1/2 (h)	F%
Rat	i.v.	0.5	0.729	0.278	/	5.1	/
Rat	p.o.	0.5	/	/	1.17	4.36	81.1
Dog	i.v.	1	3.96	0.559	/	3.56	/
Dog	p.o.	1	/	/	0.417	4.8	78.8

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

Animal Model:

Mice treated NCI-H446, NCI-H69 or IMR-32 cells^[1]
Dosage:

NCI-H446 xenograft: 10 and 20 mg/kg for 38 days
NCI-H69 xenograft: 2.5, 5, 10 and 20 mg/kg for 41 days
IMR-32 xenograft: 2.5, 5 and 10 mg/kg for 32 days
Administration:

Oral administration (p.o.)
Result:

Resulted in TGI of 78%, 97% respectively, with no significant body weight change in NCI-H446 xenograft models.
Resulted in TGI of 60%, 79%, 89%, 99% respectively, with no significant body weight change in NCI-H69 xenograft models.
Resulted in TGI of 73%, 90%, 102% respectively, with no significant body weight change in IMR-32 xenograft models.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2899209-55-1
Appearance Solid
Molecular Weight 503.97
Formel C₂₅H₂₈ClF₂N₅O₂
Color White to off-white
SMILES

ClC1=CC=CC(CN2CC[C@](C(O)=O)(CC3=CC(C)=C(F)C(NC4=CC(C)=NN4)=N3)C[C@H]2C)=C1F
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (198.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.9842 mL

9.9212 mL

19.8424 mL

5 mM

0.3968 mL

1.9842 mL

3.9685 mL

10 mM

0.1984 mL

0.9921 mL

1.9842 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (4.96 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.96 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

Verweise

[1]. Yang G, et al. Preclinical Evaluation of JAB-2485, a Potent AURKA Inhibitor with High Selectivity and Favorable Pharmacokinetic Properties. ACS Omega. 2024 May 3;9(19):21416-21425. [Content Brief]

[2]. Yang G, et, al. Abstract 1645: JAB-2485: A potent, highly selective small-molecule Aurora kinase A inhibitor that targets cell division. Cancer Res (2023) 83 (7_Supplement): 1645.

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	1.9842 mL	9.9212 mL	19.8425 mL	49.6061 mL
	5 mM	0.3968 mL	1.9842 mL	3.9685 mL	9.9212 mL
	10 mM	0.1984 mL	0.9921 mL	1.9842 mL	4.9606 mL
	15 mM	0.1323 mL	0.6614 mL	1.3228 mL	3.3071 mL
	20 mM	0.0992 mL	0.4961 mL	0.9921 mL	2.4803 mL
	25 mM	0.0794 mL	0.3968 mL	0.7937 mL	1.9842 mL
	30 mM	0.0661 mL	0.3307 mL	0.6614 mL	1.6535 mL
	40 mM	0.0496 mL	0.2480 mL	0.4961 mL	1.2402 mL
	50 mM	0.0397 mL	0.1984 mL	0.3968 mL	0.9921 mL
	60 mM	0.0331 mL	0.1654 mL	0.3307 mL	0.8268 mL
	80 mM	0.0248 mL	0.1240 mL	0.2480 mL	0.6201 mL
	100 mM	0.0198 mL	0.0992 mL	0.1984 mL	0.4961 mL

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JAB-2485

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JAB-2485

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JAB-2485 Related Classifications

HY-157396 Related Classifications