Cat. No.: HY-179572

STA-013

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STA-013 is a EphB tyrosine kinase inhibitor. STA-013 shows promising potency against EphB1 (IC₅₀ = 0.69 µM), EphB2 (IC₅₀ = 1.73 µM), and EphB4 (IC₅₀ = 1.02 µM) tyrosine kinases. STA-013 results a inhibition of the EphB phosphorylated signal, coupled with increased p-AKT/AKT signaling, to suggest insulin signaling activation. STA-013 inhibits EphB tyrosine kinase by enhancing insulin receptor beta (IRβ) signaling, and decreasing TGF-β levels in the heart. STA-013 can be used for the study of type 2 diabetes and cardiac complications (diabetic cardiomyopathy).

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Pureté: 99.18%
Formule: C₂₄H₁₇N₃O₂S
Masse moléculaire:411.48

Stockage:

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

STA-013 Chemical Structure

Size

Prix

Stock

Quantité

Amount: USD 0.00

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

Activité biologique

Description

IC₅₀ & Target^[1]

ErbB1

0.69 μM (IC₅₀)

ErbB2

1.73 μM (IC₅₀)

ErbB4

1.02 μM (IC₅₀)

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In Vitro

STA-013 (5 µM) inhibits EphB1 (54%), EphB2 (42%), EphB4 (52%), SGK1 (47%), and PKBb (43%) without affecting the rest of 140 kinases via kinome profiling assay^[1].
STA-013 (0.032-20 µM, 96 h) significantly inhibits lipid accumulation in a dose-dependent manner in the embryonic mouse 3T3-L1 cells^[1].
STA-013 (1 µM, 30 min) results a significant reduction in basal respiration, proton leak, ATP production, and non-mitochondrial oxygen consumption, increases maximal respiration and spare respiratory capacity, exhibits a significant increase in glycolysis and glycolytic capacity and reduces palmitate oxidation in 3T3-L1 cells^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC	F	C₀	T_1/2 (Metabolic)	AUC_inf	CL	V_{ss_obs}
Mice^[1]	25 mg/kg	i.p.	1126 ng/mL	0.35 h	0.158 mL/min	0.75	/	/	/	/	/
Mice^[1]	25 mg/kg	i.v.	/	/	/	/	1404 ng/mL	16.10 h	0.212 mL/min	10.50 L/h/kg	88.8 L/kg

In Vivo

STA-013 (12.5, 25 and 50 mg/kg, i.p., daily for 6 weeks) promotes weight loss, improves glucose clearance and insulin sensitivity, and enhances insulin signaling in isolated brown adipose tissue and liver in high-fat diet-induced C57BL/6J mice. In these obese mice ^[1].
STA-013 (12.5, 25 and50 mg/kg, i.p., daily for 6 weeks) induces weight loss not through reduced food intake or elevated metabolic rates in DIO mice^[1].

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

Animal Model:

HFD (for 10 weeks) induced male C57BL/6J mice (16-20 weeks old)^[1]
Dosage:

12.5, 25 and 50 mg/kg
Administration:

i.p., daily for 6 weeks
Result:

Showed a significant reduction in whole-body weight, improved glucose clearance in the IP glucose tolerance test (GTT), and insulin sensitivity in the IP insulin tolerance test (ITT).
Showed a significant reduction in the fat mass associated with preserving the lean muscle mass in HFD-obese mice.
Induced intrascapular brown adipose tissue (BAT)-specific thermogenesis in HFD obese mice.
Showed significant reduction in whole-body weight associated with reduction in the fat mass (%) as well as increase in the lean mass (%), improved glucose clearance, and restored insulin sensitivity in HFD obese mice.
Inhibited phosphorylation of ephb tyrosine kinase forward signaling in both the liver and BAT at 25 mg/kg.
Increased the p-AKT/AKT signaling, which suggests the activation of insulin signaling in BAT and liver in HFD obese mice.
Increased insr-β protein levels compared to vehicle in BAT and liver lysates.

Animal Model:

HFD (for 10 weeks) induced male C57BL/6J DIO mice (16-20 weeks old)^[1]
Dosage:

12.5, 25 and 50 mg/kg
Administration:

i.p., daily for 6 weeks
Result:

Significantly increased oxygen (VO 2 and carbon dioxide (VCO 2) consumption ) production in the light cycle.
Decreased profile in the respiratory exchange rates (RER) during the dark cycle.
Decrease in the total energy expenditure (EE) for STA- 013 treated HFD mice.
Induced weight loss occurred without a change in food intake, suggesting it was due to an elevated metabolic rate.

Chemical Information

Appearance Solid
Masse moléculaire 411.48
Formule C₂₄H₁₇N₃O₂S
Color White to light yellow
SMILES

O=C(NCC1=CC=CC2=C1C=CN2C(C3=CC=CC=C3)=O)C4=CC5=CC=CN=C5S4
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 25 mg/mL (60.76 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

2.4303 mL

12.1513 mL

24.3025 mL

5 mM

0.4861 mL

2.4303 mL

4.8605 mL

10 mM

0.2430 mL

1.2151 mL

2.4303 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)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Tareq S,et al. Discovery of pan-EphB tyrosine kinase inhibitor for metabolic syndrome sparing EphB3 signaling in mice. Pharmacol Res. 2025 Sep;219:107900. [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	2.4303 mL	12.1513 mL	24.3025 mL	60.7563 mL
	5 mM	0.4861 mL	2.4303 mL	4.8605 mL	12.1513 mL
	10 mM	0.2430 mL	1.2151 mL	2.4303 mL	6.0756 mL
	15 mM	0.1620 mL	0.8101 mL	1.6202 mL	4.0504 mL
	20 mM	0.1215 mL	0.6076 mL	1.2151 mL	3.0378 mL
	25 mM	0.0972 mL	0.4861 mL	0.9721 mL	2.4303 mL
	30 mM	0.0810 mL	0.4050 mL	0.8101 mL	2.0252 mL
	40 mM	0.0608 mL	0.3038 mL	0.6076 mL	1.5189 mL
	50 mM	0.0486 mL	0.2430 mL	0.4861 mL	1.2151 mL
	60 mM	0.0405 mL	0.2025 mL	0.4050 mL	1.0126 mL

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STA-013

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Voir tous les produits spécifiques à Isoform EGFR

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

STA-013 Related Classifications

HY-179572 Related Classifications